Updated on 2025/06/29

写真a

 
SAWADA Daisuke
 
Organization
Faculty of Medicine, Dentistry and Pharmaceutical Sciences Professor
Position
Professor
External link

Degree

  • (BLANK) ( The University of Tokyo )

Research Interests

  • 機能性分子

  • 有機金属化学

  • 医薬化学

  • 全合成

  • Organic Chemisty

  • 有機化学

Research Areas

  • Nanotechnology/Materials / Structural organic chemistry and physical organic chemistry

  • Life Science / Bioorganic chemistry

  • Life Science / Pharmaceutical chemistry and drug development sciences

Research History

  • Okayama University   Graduate School of Medicine , Dentistry and Pharmaceutical Sciences   Professor

    2013.10

      More details

  • Teikyo University   Faculty of Pharma-Science   Associate Professor

    2010.4 - 2013.9

      More details

  • Teikyo University   Faculty of Pharma-Science   Lecturer

    2006.6 - 2010.3

      More details

  • Teikyo University   Faculty of Pharma-Science   Research Assistant

    2001.4 - 2006.5

      More details

  • The University of Tokyo   Graduate School of Pharmaceutical Sciences

    2000 - 2001

      More details

Professional Memberships

 

Papers

  • Discovery of a Compound That Inhibits IRE1α S-Nitrosylation and Preserves the Endoplasmic Reticulum Stress Response under Nitrosative Stress. Reviewed International journal

    Haruna Kurogi, Nobumasa Takasugi, Sho Kubota, Ashutosh Kumar, Takehiro Suzuki, Naoshi Dohmae, Daisuke Sawada, Kam Y J Zhang, Takashi Uehara

    ACS chemical biology   2024.11

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    Inositol-requiring enzyme 1α (IRE1α) is a sensor of endoplasmic reticulum (ER) stress and drives ER stress response pathways. Activated IRE1α exhibits RNase activity and cleaves mRNA encoding X-box binding protein 1, a transcription factor that induces the expression of genes that maintain ER proteostasis for cell survival. Previously, we showed that IRE1α undergoes S-nitrosylation, a post-translational modification induced by nitric oxide (NO), resulting in reduced RNase activity. Therefore, S-nitrosylation of IRE1α compromises the response to ER stress, making cells more vulnerable. We conducted virtual screening and cell-based validation experiments to identify compounds that inhibit the S-nitrosylation of IRE1α by targeting nitrosylated cysteine residues. We ultimately identified a compound (1ACTA) that selectively inhibits the S-nitrosylation of IRE1α and prevents the NO-induced reduction of RNase activity. Furthermore, 1ACTA reduces the rate of NO-induced cell death. Our research identified S-nitrosylation as a novel target for drug development for IRE1α and provides a suitable screening strategy.

    DOI: 10.1021/acschembio.4c00403

    PubMed

    researchmap

  • 4-Hydroxy-1α,25-Dihydroxyvitamin D3: Synthesis and Structure–Function Study Reviewed

    Carole Peluso-Iltis, Noé Pierrat, Daniela Rovito, Judit Osz, Daisuke Sawada, Atsushi Kittaka, Gilles Laverny, Natacha Rochel

    Biomolecules   14 ( 5 )   551 - 551   2024.5

     More details

    Publishing type:Research paper (scientific journal)   Publisher:MDPI AG  

    The active vitamin D metabolites, 25-hydroxyvitamin D3 (25D3) and 1,25-dihydroxyvitamin D3 (1,25D3), are produced by successive hydroxylation steps and play key roles in several cellular processes. However, alternative metabolic pathways exist, and among them, the 4-hydroxylation of 25D3 is a major one. This study aims to investigate the structure–activity relationships of 4-hydroxy derivatives of 1,25D3. Structural analysis indicates that 1,4α,25(OH)3D3 and 1,4β,25(OH)3D3 maintain the anchoring hydrogen bonds of 1,25D3 and form additional interactions, stabilizing the active conformation of VDR. In addition, 1,4α,25D3 and 1,4β,25D3 are as potent as 1,25D3 in regulating the expression of VDR target genes in rat intestinal epithelial cells and in the mouse kidney. Moreover, these two 4-hydroxy derivatives promote hypercalcemia in mice at a dose similar to that of the parent compound.

    DOI: 10.3390/biom14050551

    researchmap

  • Nucleophile-Triggered π-Topological Transformation: a New Synthetic Approach to Near-Infrared-Emissive Rhodamines. Reviewed International journal

    Mei Harada, Misa Kutsuna, Taichi Kitamura, Yusuke Usui, Masayoshi Ujiki, Yuka Nakamura, Tohru Obata, Masaru Tanioka, Masanobu Uchiyama, Daisuke Sawada, Shinichiro Kamino

    Chemistry (Weinheim an der Bergstrasse, Germany)   e202301969   2023.7

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    We describe a π-topological transformation-based synthetic method for the preparation of a new type of near-infrared (NIR)-emissive rhodamine dye called Polymethine-embedded Rhodamine Fluorophore (PeR Fluor). In contrast to conventional NIR-emissive dyes that require tedious synthetic steps and/or a high cost, linear fully π-conjugated PeR Fluor can be regioselectively prepared in one step by mixing different nucleophiles with ABPXs, a family of rhodamines with a cross-conjugated structure. PeR Fluor exhibits bright NIR fluorescence emission and high photostability owing to the cooperative π-electron system of rhodamines and polymethine scaffolds. Large bathochromic shifts of the absorption and fluorescence emission maxima can be achieved by modifying the N-substituted group to obtain NIR-absorbing/emitting PeR Fluor. We also demonstrate the stimulus-responsive functionality of PeR Fluor through the addition of chemicals (acid/base), which shows switchable NIR and visible fluorescence response. Our π-topological transformation-based synthetic method is a promising approach to produce new functionalized rhodamine dyes.

    DOI: 10.1002/chem.202301969

    PubMed

    researchmap

  • First Total Synthesis of Reassigned Echinosulfonic Acid D Reviewed

    Takumi Abe, Ren Nakajima, Toshiki Yamashiro, Daisuke Sawada

    Journal of Natural Products   2022.8

     More details

    Language:English   Publishing type:Research paper (scientific journal)   Publisher:American Chemical Society ({ACS})  

    DOI: 10.1021/acs.jnatprod.2c00559

    researchmap

  • Indole Editing Enabled by HFIP‐Mediated Ring‐Switch Reactions of 3‐Amino‐2‐Hydroxyindolines Reviewed

    Takumi Abe, Toshiki Yamashiro, Kaho Shimizu, Daisuke Sawada

    Chemistry – A European Journal   2022.5

     More details

    Publishing type:Research paper (scientific journal)   Publisher:Wiley  

    DOI: 10.1002/chem.202201113

    researchmap

  • Chemo- and Site-Selective Replacement of N-Terminal Carbamates in Peptides Reviewed

    Miho Ibara, Takumi Abe, Daisuke Sawada

    Organic Letters   142nd   2022.3

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/acs.orglett.2c00370

    J-GLOBAL

    researchmap

  • Synthesis of 2-monosubstituted indolin-3-ones by cine-substitution of 3-azido-2-methoxyindolines Reviewed

    Toshiki Yamashiro, Takumi Abe, Daisuke Sawada

    Organic Chemistry Frontiers   2022

     More details

    Publishing type:Research paper (scientific journal)   Publisher:Royal Society of Chemistry (RSC)  

    We have developed an efficient reaction of 3-azido-2-methoxyindolines with <italic>O</italic>-nucleophiles in the presence of a Lewis acid, affording 2-monoacyloxy or alkoxy indolin-3-ones.

    DOI: 10.1039/d2qo00048b

    researchmap

  • Synthesis of α-substituted indolylacetamide using acetonitriles as acetamide enolate equivalents through O-transfer reactions. Reviewed International journal

    Takumi Abe, Kenta Noda, Daisuke Sawada

    Chemical communications (Cambridge, England)   57 ( 61 )   7493 - 7496   2021.7

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1039/d1cc02821a

    Web of Science

    Scopus

    PubMed

    researchmap

  • Cis-3-Azido-2-Methoxyindolines as Safe and Stable Precursors to Overcome the Instability of Fleeting 3-Azidoindoles Reviewed

    Toshiki Yamashiro, Takumi Abe, Masaru Tanioka, Shinichiro Kamino, Daisuke Sawada

    Chemical Communications   2021

     More details

    Publishing type:Research paper (scientific journal)   Publisher:Royal Society of Chemistry (RSC)  

    Use of 3-azidoindoles in organic synthesis remains difficult task owing to their instabilities. Herein, we report a general and concise approach for tackling this problem by using 3-azidoindole surrogates. The...

    DOI: 10.1039/d1cc06033c

    researchmap

  • Morpholine-Substituted Rhodamine Analog with Multi-Configurational Switches for Optical Sensing of pH Gradient under Extreme Acidic Environments. Reviewed International journal

    Natsumi Koga, Masaru Tanioka, Shinichiro Kamino, Daisuke Sawada

    Chemistry (Weinheim an der Bergstrasse, Germany)   27 ( 11 )   3761 - 3765   2020.11

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1002/chem.202004254

    Web of Science

    Scopus

    PubMed

    researchmap

  • Stepwise structural and fluorescent colour conversion in rhodamine analogues based on light and acid stimulations Reviewed

    Masaru Tanioka, Shinichiro Kamino, Natsumi Koga, Daisuke Sawada

    JOURNAL OF MATERIALS CHEMISTRY C   8 ( 2 )   543 - 549   2020.1

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1039/c9tc05054j

    Web of Science

    Scopus

    researchmap

  • Efficient and practical synthesis of N-acetyl enamides from ketoximes by unique iron catalytic system Reviewed

    Takahiro Kunishige, Daisuke Sawada

    TETRAHEDRON LETTERS   60 ( 24 )   1562 - 1565   2019.6

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.tetlet.2019.05.006

    Web of Science

    Scopus

    researchmap

  • Synthesis of a tetracyclic aminobenzimidazole derivative via tandem cyclization of triphenylguanidine Reviewed

    Yuki Akamatsu, Shinichiro Kamino, Daisuke Sawada

    Heterocycles   99 ( 2 )   815 - 819   2019

     More details

    Publishing type:Research paper (scientific journal)  

    DOI: 10.3987/COM-18-S(F)61

    Scopus

    researchmap

  • Syntheses and acid-stimulus responsiveness of aminobenzopyranoxanthene spiroethers Reviewed

    Ryosuke Hosoda, Shinichiro Kamino, Masashi Ueda, Daisuke Sawada

    Heterocycles   99 ( 2 )   820 - 824   2019

     More details

    Publishing type:Research paper (scientific journal)  

    DOI: 10.3987/COM-18-S(F)66

    Scopus

    researchmap

  • Stable Thiele's Hydrocarbon Derivatives Exhibiting Near-Infrared Absorption/Emission and Two-Step Electrochromism. Reviewed International journal

    Yuta Okamoto, Masaru Tanioka, Atsuya Muranaka, Kazunori Miyamoto, Tetsuya Aoyama, Xingmei Ouyang, Shinichiro Kamino, Daisuke Sawada, Masanobu Uchiyama

    Journal of the American Chemical Society   140 ( 51 )   17857 - 17861   2018.12

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/jacs.8b11092

    Web of Science

    Scopus

    PubMed

    researchmap

  • Effects of 2-substitution on 14-epi-19-nortachysterol-mediated biological events: Based on synthesis and X-ray co-crystallographic analysis with human vitamin D receptor Reviewed

    Daisuke Sawada, Shinji Kakuda, Akiko Takeuchi, Fumihiro Kawagoe, Midori Takimoto-Kamimura, Atsushi Kittaka

    ORGANIC & BIOMOLECULAR CHEMISTRY   16 ( 14 )   2448 - 2455   2018.3

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1039/c8ob00158h

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis of Aminobenzopyranoxanthenes with Nitrogen-Containing Fused Rings Reviewed

    Natsumi Fukino, Shinichiro Kamino, Minami Takahashi, Daisuke Sawada

    JOURNAL OF ORGANIC CHEMISTRY   82 ( 24 )   13626 - 13631   2017.12

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/acs.joc.7b02290

    Web of Science

    Scopus

    PubMed

    researchmap

  • Direct C-H substitution reaction of anilides using hypervalent iodine and their regioselective issues Reviewed

    Kohki Yamamoto, Shinichiro Kamino, Daisuke Sawada

    TETRAHEDRON LETTERS   58 ( 41 )   3936 - 3938   2017.10

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.tetlet.2017.08.079

    Web of Science

    Scopus

    researchmap

  • Synthesis of 2 alpha- and 2 beta-(3-hydroxypropyl)-7,8-cis-14-epi-1 alpha,25-dihydroxy-19-norvitamin D-3 and their biological activity Reviewed

    Daisuke Sawada, Eiji Ochiai, Akiko Takeuchi, Shinji Kakuda, Midori Kamimura-Takimoto, Fumihiro Kawagoe, Atsushi Kittaka

    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY   173   79 - 82   2017.10

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.jsbmb.2016.09.007

    Web of Science

    Scopus

    PubMed

    researchmap

  • Novel screening system for high-affinity ligand of heredity vitamin D-resistant rickets-associated vitamin D receptor mutant R274L using bioluminescent sensor Reviewed

    Hiroki Mano, Miyu Nishikawa, Kaori Yasuda, Shinichi Ikushiro, Nozomi Saito, Daisuke Sawada, Shinobu Honzawa, Masashi Takano, Atsushi Kittaka, Toshiyuki Sakaki

    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY   167   61 - 66   2017.3

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.jsbmb.2016.11.008

    Web of Science

    Scopus

    PubMed

    researchmap

  • SYNTHESES AND PHOTOPHYSICAL PROPERTIES OF AMINOBENZOPYRANOXANTHENE DYES CONTAINING VARIOUS ALKYL CHAINS AT AMINE MOIETIES Reviewed

    Shinichiro Kamino, Masaru Tanioka, Daisuke Sawada, Shuichi Enomoto

    HETEROCYCLES   95 ( 2 )   1167 - 1176   2017.1

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.3987/COM-16-S(S)65

    Web of Science

    Scopus

    researchmap

  • Water-tunable solvatochromic and nanoaggregate fluorescence: dual colour visualisation and quantification of trace water in tetrahydrofuran Reviewed

    Masaru Tanioka, Shinichiro Kamino, Atsuya Muranaka, Yoshinao Shirasaki, Yousuke Ooyama, Masashi Ueda, Masanobu Uchiyama, Shuichi Enomoto, Daisuke Sawada

    PHYSICAL CHEMISTRY CHEMICAL PHYSICS   19 ( 2 )   1209 - 1216   2017.1

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1039/c6cp06808a

    Web of Science

    Scopus

    PubMed

    researchmap

  • Fused-Fluoran Leuco Dyes with Large Color-Change Derived from Two-Step Equilibrium: iso-Aminobenzopyranoxanthenes Reviewed

    Yoshinao Shirasaki, Yuta Okamoto, Atsuya Muranaka, Shinichiro Kamino, Daisuke Sawada, Daisuke Hashizume, Masanobu Uchiyama

    JOURNAL OF ORGANIC CHEMISTRY   81 ( 23 )   12046 - 12051   2016.12

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/acs.joc.6b02403

    Web of Science

    Scopus

    researchmap

  • Revisiting the 7,8-cis-vitamin D3 derivatives: synthesis, evaluating the biological activity, and study of the binding configuration Reviewed

    Daisuke Sawada, Shinji Kakuda, Midori Kamimura-Takimoto, Akiko Takeuchi, Yotaro Matsumoto, Atsushi Kittaka

    Tetrahedron   72 ( 22 )   2838 - 2848   2016.4

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.tet.2016.03.081

    Web of Science

    Scopus

    researchmap

  • Reversible Near-Infrared/Blue Mechanofluorochromism of Aminobenzopyranoxanthene Reviewed

    Masaru Tanioka, Shinichiro Kamino, Atsuya Muranaka, Yousuke Ooyama, Hiromi Ota, Yoshinao Shirasaki, Jun Horigome, Masashi Ueda, Masanobu Uchiyama, Daisuke Sawada, Shuichi Enomoto

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   137 ( 20 )   6436 - 6439   2015.5

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/jacs.5b00877

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis and metabolic studies of 1 alpha,2 alpha,25-, 1 alpha,4 alpha,25-and 1 alpha,4 beta,25-trihydroxyvitamin D-3 Reviewed

    Masashi Takano, Daisuke Sawada, Kaori Yasuda, Miyu Nishikawa, Akiko Takeuchi, Ken-ichiro Takagi, Kyohei Horie, G. Satyanarayana Reddy, Tai C. Chen, Toshiyuki Sakaki, Atsushi Kittaka

    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY   148   34 - 37   2015.4

  • ビタミンD受容体リガンドの創製 Invited

    橘高敦史, 澤田大介

    ファルマシア   51 ( 3 )   196 - 200   2015.3

     More details

    Language:Japanese   Publishing type:Research paper (scientific journal)  

    researchmap

  • SYNTHESIS AND PRELIMINARY BIOLOGICAL EVALUATION OF 2-[3-(TETRAZOLYL)PROPYL]-1 alpha,25-DIHYDROXY-19-NORVITAMIN D-3 Invited Reviewed

    Masashi Takano, Erika Higuchi, Kazunari Higashi, Keisuke Hirano, Akiko Takeuchi, Daisuke Sawada, Atsushi Kittaka

    HETEROCYCLES   90 ( 2 )   1274 - 1287   2015.1

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.3987/COM-14-S(K)108

    Web of Science

    Scopus

    researchmap

  • Synthesis and Properties of 14-epi-1 alpha,25-Dihydroxy-19-Nortachysterol and its 2-Substituted Derivatives Invited Reviewed

    Daisuke Sawada, Atsushi Kittaka

    CURRENT TOPICS IN MEDICINAL CHEMISTRY   14 ( 21 )   2454 - 2459   2014.12

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.2174/1568026615666141208103741

    Web of Science

    Scopus

    PubMed

    researchmap

  • Design and synthesis of 2α-(tetrazolylethyl)-1α,25-dihydroxyvitamin D3 as a high affinity ligand for vitamin D receptor. Reviewed

    Matsuo M, Hasegawa A, Takano M, Saito H, Kakuda S, Takagi K, Ochiai E, Horie K, Takimoto-Kamimura M, Takenouchi K, Sawada D, Kittaka A

    The Journal of steroid biochemistry and molecular biology   144PA ( PART A )   201 - 203   2014.10

  • Synthesis and biological activity of 1α,2α,25-trihydroxyvitamin D3: active metabolite of 2α-(3-hydroxypropoxy)-1α,25-dihydroxyvitamin D3 by human CYP3A4. Reviewed

    Takano M, Ohya S, Yasuda K, Nishikawa M, Takeuchi A, Sawada D, Sakaki T, Kittaka A

    Chemical & pharmaceutical bulletin   62 ( 2 )   182 - 184   2014

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1248/cpb.c13-00646

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo. Reviewed

    Matsuo M, Hasegawa A, Takano M, Saito H, Kakuda S, Chida T, Takagi K, Ochiai E, Horie K, Harada Y, Takimoto-Kamimura M, Takenouchi K, Sawada D, Kittaka A

    ACS medicinal chemistry letters   4 ( 7 )   671 - 674   2013.7

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/ml400098w

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis of 14-epi-2α-hydroxypropoxy-1α,25-dihydroxy-19-nortachysterol and its hVDR binding. Reviewed

    Sawada D, Tsukuda Y, Saito H, Takagi K, Kakuda S, Takimoto-Kamimura M, Ochiai E, Takenouchi K, Kittaka A

    The Journal of steroid biochemistry and molecular biology   136 ( 1 )   27 - 29   2013.7

  • Potent 19-norvitamin D analogs for prostate and liver cancer therapy. Reviewed

    Kittaka A, Yoshida A, Chiang KC, Takano M, Sawada D, Sakaki T, Chen TC

    Future medicinal chemistry   4 ( 16 )   2049 - 2065   2012.10

  • C15-functionalized 16-ene-1α,25-dihydroxyvitamin D3 is a new vitamin D analog with unique biological properties. Reviewed

    Kumagai G, Takano M, Shindo K, Sawada D, Saito N, Saito H, Kakuda S, Takagi K, Takimoto-Kamimura M, Takenouchi K, Chen TC, Kittaka A

    Anticancer research   32 ( 1 )   311 - 317   2012.1

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    Web of Science

    Scopus

    PubMed

    researchmap

  • The difference between 14-epi-previtamin D3 and 14-epi-19-norprevitamin D3: their synthesis and binding affinity for human VDR. Reviewed

    Sawada D, Katayama T, Tsukuda Y, Saito N, Saito H, Kakuda S, Takimoto-Kamimura M, Takenouchi K, Kittaka A

    Anticancer research   32 ( 1 )   319 - 326   2012.1

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis and biological activities of 1α,4α,25- and 1α,4β,25-trihydroxyvitamin D(3) and their metabolism by human CYP24A1 and UDP-glucuronosyltransferase. Reviewed

    Sawada D, Tsukuda Y, Yasuda K, Sakaki T, Saito H, Takagi K, Takenouchi K, Chen TC, Reddy GS, Kittaka A

    Chemical & pharmaceutical bulletin   60 ( 10 )   1343 - 1346   2012

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1248/cpb.c12-00526

    Web of Science

    Scopus

    PubMed

    researchmap

  • A Multivalent Probe for AI-2 Quorum-Sensing Receptors Reviewed

    Amanda L. Garner, Junguk Park, Joseph S. Zakhari, Colin A. Lowery, Anjali Kumari Struss, Daisuke Sawada, Gunnar F. Kaufmann, Kim D. Janda

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   133 ( 40 )   15934 - 15937   2011.10

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/ja207556d

    Web of Science

    Scopus

    PubMed

    researchmap

  • New C15-substituted active vitamin D3. Reviewed

    Shindo K, Kumagai G, Takano M, Sawada D, Saito N, Saito H, Kakuda S, Takagi K, Ochiai E, Horie K, Takimoto-Kamimura M, Ishizuka S, Takenouchi K, Kittaka A

    Organic letters   13 ( 11 )   2852 - 2855   2011.6

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/ol200828s

    Web of Science

    Scopus

    PubMed

    researchmap

  • Development of 14-epi-19-Nortachysterol and Its Unprecedented Binding Configuration for the Human Vitamin D Receptor Reviewed

    Daisuke Sawada, Yuya Tsukuda, Hiroshi Saito, Shinji Kakuda, Midori Takimoto-Kamimura, Eiji Ochiai, Kazuya Takenouchi, Atsushi Kittaka

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   133 ( 18 )   7215 - 7221   2011.5

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/ja201481j

    Web of Science

    Scopus

    PubMed

    researchmap

  • Medicinal Chemistry as a Conduit for the Modulation of Quorum Sensing Reviewed

    Colin A. Lowery, Nicholas T. Salzameda, Daisuke Sawada, Gunnar F. Kaufmann, Kim D. Janda

    JOURNAL OF MEDICINAL CHEMISTRY   53 ( 21 )   7467 - 7489   2010.11

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/jm901742e

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis of 2- and 2-Substituted-14-epi-previtamin D3 and Their Genomic Activity Reviewed

    Daisuke Sawada, Tomoyuki Katayama, Yuya Tsukuda, Nozomi Saito, Hiroshi Saito, Ken-ichiro Takagi, Eiji Ochiai, Seiichi Ishizuka, Kazuya Takenouchi, Atsushi Kittaka

    Tetrahedron   66 ( 29 )   5407 - 5423   2010

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.tet.2010.05.028

    Web of Science

    Scopus

    researchmap

  • Studies on the Synthesis and Metabolism of 14-epi-2-(3-Hydroxypropyl)-19-norvitamin D3 and Its 2-Isomer Reviewed

    Atsushi Kittaka, Hideki Hara, Kaori Yasuda, Masashi Takano, Midori A. Arai, Daisuke Sawada, Hiroshi Saito, Kazuya Takenouchi, Tai C. Chen, Toshiyuki Sakaki

    Heterocycles   82 ( 1 )   649 - 661   2010

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.3987/COM-10-S(E)40

    Web of Science

    researchmap

  • Synthesis of 2-Substituted-14-epi-previtamin D3 and Testing of Its Genomic Activity Reviewed

    Daisuke Sawada, Yuya Tsukuda, Hiroshi Saito, Ken-ichiro Takagi, Eiji Ochiai, Seiichi Ishizuka, Kazuya Takenouchi, Atsushi Kittaka

    J. Steroid Biochem. Mol. Biol.   121 ( 1-2 )   20 - 24   2010

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.jsbmb.2010.02.035

    Web of Science

    Scopus

    PubMed

    researchmap

  • Revisiting AI-2 Quorum Sensing Inhibitors: Direct Comparison of Alkyl-DPD Analogues and a Natural Product Fimbrolide Reviewed

    Colin A. Lowery, Takumi Abe, Junguk Park, Lisa M. Eubanks, Daisuke Sawada, Gunnar F. Kaufmann, Kim D. Janda

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   131 ( 43 )   15584 - +   2009.11

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/ja9066783

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis of 2alpha-substituted-14-epi-previtamin D3 and its genomic activity. Reviewed

    Sawada D, Katayama T, Tsukuda Y, Saito N, Takano M, Saito H, Takagi K, Ochiai E, Ishizuka S, Takenouchi K, Kittaka A

    Bioorganic & medicinal chemistry letters   19 ( 18 )   5397 - 5400   2009.9

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.bmcl.2009.07.112

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis and biological activities of 14-epi-MART-10 and 14-epi-MART-11: implications for cancer and osteoporosis treatment. Reviewed

    Kittaka A, Hara H, Takano M, Sawada D, Arai MA, Takagi K, Chida T, Harada Y, Saito H, Takenouchi K, Ishizuka S, Hayashi K, Ikushiro S, Sakaki T, Sugiura T, Chen TC

    Anticancer research   29 ( 9 )   3563 - 3569   2009.9

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    Web of Science

    Scopus

    PubMed

    researchmap

  • Synthesis and Biological Evaluation of 4-Substituted Vitamin D and 14-Epi-Previtamin D Analogs Reviewed

    Daisuke Sawada, Yuya Tsukuda, Hiroshi Saito, Ken-ichiro Takagi, Kyouhei Horie, Eiji Ochiai, Kazuya Takenouchi, Atsushi Kittaka

    Chem. Pharm. Bull.   57 ( 12 )   1431 - 1433   2009

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1248/cpb.57.1431

    Web of Science

    Scopus

    PubMed

    researchmap

  • Novel synthesis of oligosaccharides linked with carbamate and urea bonds utilizing modified Curtius rearrangement Reviewed

    Daisuke Sawada, Shinya Sasayama, Hideyo Takahashi, Shiro Ikegami

    TETRAHEDRON   64 ( 37 )   8780 - 8788   2008.9

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/j.tet.2008.06.089

    Web of Science

    Scopus

    researchmap

  • Novel synthesis of carbamate-linked oligosaccharides by a modified curtius rearrangement Reviewed

    Daisuke Sawada, Shinya Sasayama, Hideyo Takahashi, Shiro Ikegami

    EUROPEAN JOURNAL OF ORGANIC CHEMISTRY   2007 ( 7 )   1064 - 1068   2007.2

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1002/ejoc.200600993

    Web of Science

    Scopus

    researchmap

  • Short-step synthesis of 5-thio-l-hexopyranoses from d-glyconothio-O-lactones Reviewed

    Daisuke Sawada, Shinya Sasayama, Hideyo Takahashi, Shiro Ikegami

    Heterocycles   66 ( 1 )   441 - 451   2005.12

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.3987/COM-05-S(K)52

    Scopus

    researchmap

  • Synthesis of N-protected azaoligosaccharides and their cyclic derivatives Reviewed

    Daisuke Sawada, Hideyo Takahashi, Moto Shiro, Shiro Ikegami

    Tetrahedron Letters   46 ( 14 )   2399 - 2403   2005.4

     More details

    Language:English   Publishing type:Research paper (scientific journal)   Publisher:Elsevier Ltd  

    DOI: 10.1016/j.tetlet.2005.02.057

    Scopus

    researchmap

  • Efficient synthesis of 1-deoxy-azasugars as useful synthetic tools Reviewed

    Daisuke Sawada, Hideyo Takahashi, Shiro Ikegami

    Tetrahedron Letters   44 ( 15 )   3085 - 3088   2003.4

     More details

    Language:English   Publishing type:Research paper (scientific journal)   Publisher:Elsevier Ltd  

    DOI: 10.1016/S0040-4039(03)00512-4

    Scopus

    researchmap

  • A new method for formacetal linkage formation: Protection of alcohols, phenols and carboxylic acids Reviewed

    Daisuke Sawada, Yukishige Ito

    Tetrahedron Letters   42 ( 13 )   2501 - 2504   2001.3

     More details

    Publishing type:Research paper (scientific journal)  

    DOI: 10.1016/S0040-4039(01)00212-X

    Scopus

    researchmap

  • Enantioselective total synthesis of epothilones A and B using multifunctional asymmetric catalysis Reviewed

    D Sawada, M Kanai, M Shibasaki

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   122 ( 43 )   10521 - 10532   2000.11

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1021/ja002024b

    Web of Science

    Scopus

    researchmap

  • Enantioselective total synthesis of epothilone A using multifunctional asymmetric catalyses Reviewed

    D Sawada, M Shibasaki

    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION   39 ( 1 )   209 - +   2000

     More details

    Language:English   Publishing type:Research paper (scientific journal)  

    DOI: 10.1002/(SICI)1521-3773(20000103)39:1<209::AID-ANIE209>3.0.CO;2-F

    Web of Science

    Scopus

    researchmap

  • A new bifunctional asymmetric catalysis: An efficient catalytic asymmetric cyanosilylation of aldehydes Reviewed

    Y Hamashima, D Sawada, M Kanai, M Shibasaki

    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY   121 ( 11 )   2641 - 2642   1999.3

     More details

  • Novel phorbol analogs which bind to protein kinase C (PKC) without activation Reviewed

    K. Sugita, D. Sawada, M. Sodeoka, H. Sasai, M. Shibasaki

    Chemical and Pharmaceutical Bulletin   44 ( 2 )   463 - 465   1996

     More details

    Publishing type:Research paper (scientific journal)  

    DOI: 10.1248/cpb.44.463

    Scopus

    PubMed

    researchmap

  • 4 SYNTHESIS TOWAED ADVANCED ANALOG OF PMA AND EVALUATION OF ITS BIOLOGICAL ACTIVITY

    SUGITA Kazuyuki, SAWADA Daisuke, SODEOKA Mikiko, SASAI Hiroaki, SHIBASAKI Masakatsu

    Symposium on the Chemistry of Natural Products, symposium papers   ( 37 )   19 - 24   1995.9

     More details

    Language:Japanese   Publisher:Symposium on the chemistry of natural products  

    The enzyme protein kinase C (PKC) is thought to play a major role in cellular signal transduction and has been shown to exist as several isoforms. PKC is activated in cells by diacylglycerol and other diverse tumor promotors such as phorbol 12-myristate-13-acetate (1; PMA). Computer modeling studies on PMA have suggested that carbonyl group at C-3, hydroxyl groups at C-4, C-9, and C-20, and a long-chain hydrophobic portion at C-12 would be important to bind with PKC. However these structural hypotheses have not been confirmed by determining the actual PKC binding affinity or activity relationships of such substituted phorbols. We report here the entire stereospecific syntheses of phorbol analogs with the proposed necessary structural features in PKC activation. In particular, these include the syntheses of the analogs 7 and 10 having long-chain hydrophobic moieties at C-12 of their phorbol C-rings. The key intermediate 18 for the synthesis of these analogs is prepared from (+)-3-carene in a stereocontrolled manner. For the synthesis of 10, treatment of 18 with the phosphonate carbanion generated from 19 resulted in stereospecific formation of the E-stereoisomer of 20. DIBAH reduction of 20 and protection of the resulting primary alcohol, as its tert-butyldiphenylsilyl ether, yielded 21. A three-step series of reactions involving tosylation, iodide substitution, and nitration gave 22. The next crucial step was intramolecular cyclization of 22 to the corresponding isoxazolin 23, which was subsequently hydrogenated to the hydroxy ketone 24 in 85% yield (2 steps). Internal cerium alkoxide assisted propynylation of 24 was then followed by oxidation and conversion of the resulting intermediate into the ethyl-ketone 26. Intramolecular aldol cyclization of 26 and dehydration of the resulting aldol mixture in one-pot, followed by deprotection of the silyl ethers, gave the analog 9. Its allylic alcohol functionality was protected as its trityl ether, and the long-chain myristate group was then introduced at C-12. Selective deprotection of the trityl group of the resulting intermediate afforded the phorbol analog 10. The remaining hydrophobic analog 7 was obtained from 18 using similar methods to those used in the conversion of 18 to 10. The in vitro binding affinity of the phorbol analogs 7 and 10, relative to that of PMA (1), was then evaluated. The analog 7 proved to be very weak with respect to its affinity to bind to PKC, and an approximate 100 fold concentration of 10 was required. These results suggested that either the additional methyl and/or the acetoxyl groups at C-11 and C-13 respectively of 1 are also responsible for its high binding affinity to PKC. They may also be attributed to the presence of too much hydrophobic character due to the long chain at C-12 of the deacetoxy analog 10 resulting in a different hydrophobic interaction with phosphatidyl serine or PKC. In fact, an analog which has octanoyl group at C-12 shows higher binding affinity than that of 10.

    DOI: 10.24496/tennenyuki.37.0_19

    CiNii Article

    CiNii Books

    researchmap

▼display all

Books

  • 有機化学

    新スタ薬シリーズ編集委員会( Role: Contributor)

    東京化学同人  2024.7  ( ISBN:9784807917365

     More details

    Total pages:xiv, 472p   Language:Japanese

    CiNii Books

    researchmap

MISC

  • 小胞体ストレスセンサーIRE1αを標的としたS-ニトロシル化阻害薬の開発

    黒木春那, ZHANG Kam, KUMAR Ashutosh, 阿部匠, 澤田大介, 上原孝

    日本酸化ストレス学会学術集会プログラム・抄録集   77th   2024

  • IRE1α特異的酸化修飾阻害薬の開発とその抗細胞死効果

    黒木春那, ZHANG Kam, KUMAR Ashutosh, 阿部匠, 澤田大介, 上原孝

    日本薬理学雑誌   159 ( Supplement )   2024

  • Identification and evaluation of a compound that specifically inhibits oxidative modification of IRE1α

    黒木春那, ZHANG Kam Y.J., 阿部匠, 澤田大介, 上原孝

    日本薬学会年会要旨集(Web)   143rd   2023

  • Characterization of a specific inhibitor of DNMT3B S-nitrosylation

    伊藤嘉崇, 山元黎奈, 野村亮輔, 阿部匠, 澤田大介, 上原孝

    日本薬学会年会要旨集(Web)   143rd   2023

  • Synthesis of 2-arylindoles by the dehydrative skeletal rearrangement and its application

    清水香帆, 阿部匠, 谷岡卓, 神野伸一郎, 澤田大介

    日本薬学会年会要旨集(Web)   142nd   2022

  • Development and application of indolyl azide equivalents based on the stabilization by O-Nβ bonding

    山城寿樹, 阿部匠, 谷岡卓, 神野伸一郎, 澤田大介

    日本薬学会年会要旨集(Web)   142nd   2022

  • アジドインドリンの開発とその応用

    山城寿樹, 阿部匠, 谷岡卓, 神野伸一郎, 澤田大介

    反応と合成の進歩シンポジウム講演要旨集   48th   2022

  • チオアミドを用いたペプチドN末端カルバメート保護基変換反応の開発

    茨実穂, 阿部匠, 澤田大介

    反応と合成の進歩シンポジウム講演要旨集   47th   2021

  • Synthesis of Indolyacetamides by Alkylation・Cyclization・O-Transfer Reactions

    阿部匠, 野田健太, 澤田大介

    日本薬学会年会要旨集(Web)   141st   2021

  • Synthesis of benzothiazole-linked polycyclic compounds via intramolecular C-H bond activation - cyclization and application to macrocyclic compounds

    和久夢, 阿部匠, 澤田大介

    日本薬学会年会要旨集(Web)   141st   2021

  • 二重極性転換型インドール試薬の開発と芳香族求核置換反応への応用

    平尾誠弥, 阿部匠, 澤田大介

    反応と合成の進歩シンポジウム講演要旨集   47th   2021

  • ベンゾチアゾール連結型大環状化合物の合成研究

    和久夢, 木全桃子, 阿部匠, 澤田大介

    反応と合成の進歩シンポジウム講演要旨集   47th   2021

  • Development of chromic molecule that can change color and absorption/fluorescence wavelengths largely in response to external stimuli Reviewed

    Shinichiro Kamino, Masaru Tanioka, Daisuke Sawada

    Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry   76 ( 10 )   1066 - 1075   2018

     More details

    Publishing type:Book review, literature introduction, etc.  

    DOI: 10.5059/yukigoseikyokaishi.76.1066

    Scopus

    researchmap

  • 2. 7,8-cis-19-Norvitamin D_3の合成とVDR結合および7,8-cis-vitamin D_3の化学的性質(研究発表,第348回会議研究発表要旨,脂溶性ビタミン総合研究委員会)

    澤田 大介, 松本 洋太郎, 川越 文裕, 竹内 明子, 角田 真二, 上村 みどり, 橘高 敦史

    ビタミン   90 ( 2 )   84 - 85   2016.2

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 8,9‐ジヒドロ‐19‐ノルタキステロール誘導体の合成と生物活性評価

    松本洋太郎, 澤田大介, 竹内明子, 橘高敦史

    反応と合成の進歩シンポジウム講演要旨集   40th   27   2014.10

     More details

    Language:Japanese  

    J-GLOBAL

    researchmap

  • 8,9‐ジヒドロ‐19‐ノルタキステロールの合成研究

    松本洋太郎, 山田徹, 森幸樹, 澤田大介, 橘高敦史

    日本薬学会関東支部大会講演要旨集   58th   189   2014.9

     More details

    Language:Japanese  

    J-GLOBAL

    researchmap

  • 2-II-19 2α位にテトラゾールプロピル基を有する19-ノル型ビタミンD_3の合成と生物活性評価(一般演題要旨,第66回大会講演要旨)

    高野 真史, 樋口 恵理香, 竹内 明子, 澤田 大介, 橘高 敦史

    ビタミン   88 ( 4 )   244 - 244   2014.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 14‐エピ‐8,9‐ジヒドロ‐1α,25‐ジヒドロキシ‐19‐ノルタキステロールの合成

    澤田大介, 松本洋太郎, 竹内明子, 橘高敦史

    日本薬学会年会要旨集(CD-ROM)   134th   ROMBUNNO.29AMS-054   2014

     More details

    Language:Japanese  

    J-GLOBAL

    researchmap

  • 2. 2α-アゾールエチル基を有する1α, 25-ジヒドロキシビタミンD_3の合成と生物活性評価(研究発表,第340回会議研究発表要旨,脂溶性ビタミン総合研究委員会)

    橘高 敦史, 堀江 恭平, 上村 みどり, 竹之内 一弥, 松尾 実紀, 長谷川 麻美, 高野 真史, 澤田 大介, 齋藤 博, 角田 真二, 高木 健一郎, 落合 鋭士

    ビタミン   87 ( 11 )   652 - 652   2013

     More details

    Language:Japanese   Publisher:公益社団法人 日本ビタミン学会  

    DOI: 10.20632/vso.87.11_652

    CiNii Article

    researchmap

  • 2-III-6 14-エピタキステロール類の合成とVDR結合様式の解明(一般演題要旨,第65回大会講演要旨)

    澤田 大介, 堀江 恭平, 落合 鋭士, 竹内 明子, 角田 真二, 上村 みどり, 橘高 敦史

    ビタミン   87 ( 4 )   220 - 220   2013

     More details

    Language:Japanese   Publisher:公益社団法人 日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 2alpha-(3-ヒドロキシプロピル)-lalpha,25-ジヒドロキシ-19-ノルビタミンD_3(MART-10)とその類縁体の合成と抗がん活性等(研究発表,第336回会議研究発表要旨,脂溶性ビタミン総合研究委員会)

    高野 真史, 澤田 大介, 橘高 敦史, 高木 健一郎, 千田 貴之, 原田 善文, 齋藤 博, 山本 恵子, 榊 利之, Chiang Kun-Chun, Zheng Shasha, Flanagan John N, Chen Tai C

    ビタミン   86 ( 12 )   694 - 696   2012.12

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    DOI: 10.20632/vso.86.12_694

    CiNii Article

    CiNii Books

    researchmap

  • ヒト由来CYP24A1抵抗性ビタミンD誘導体合成とATRA耐性APL細胞分化誘導(一般演題要旨,日本ビタミン学会第64回大会講演要旨)

    高野 真史, 松本 直樹, 林 恵子, 生城 真一, 榊 利之, 角田 真二, 高木 健一郎, 落合 鋭士, 堀江 恭平, 上村 みどり, 澤田 大介, 野尻 久雄, 橘高 敦史

    ビタミン   86 ( 4 )   243 - 243   2012.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 14-エピ-19-ノルタキステロールの合成とVDRリガンド骨格としての可能性(第332回会議研究発表要旨,脂溶性ビタミン総合研究委員会)

    澤田 大介, 佃 勇也, 橘高 敦史, 齋藤 博, 角田 真二, 上村 みどり, 竹之内 一弥

    ビタミン   86 ( 3 )   181 - 182   2012.3

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    DOI: 10.20632/vso.86.3_181

    CiNii Article

    researchmap

  • EVALUATION AND CHARACTERIZATION OF 14-EPI-19-NORTACHYSTEROL ANALOGS FROM 14-EPI-19-NORPREVITAMIN D-3 Reviewed

    D. Sawada, Y. Tsukuda, H. Saito, K. Takagi, S. Kakuda, M. T. Kamimura, K. Takenouchi, A. Kittaka

    ANTICANCER RESEARCH   31 ( 4 )   1501 - 1501   2011.4

     More details

    Language:English   Publishing type:Research paper, summary (international conference)  

    Web of Science

    researchmap

  • SYNTHESIS OF C15-MODIFIED 16-ENE-ACTIVE VITAMIN D-3 ANALOGS FOR THE RECEPTOR-LIGAND INTERACTION STUDIES Reviewed

    A. Kittaka, G. Kumagai, M. Takano, D. Sawada, H. Saito, S. Kakuda, K. Takagi, E. Ochiai, K. Horie, K. Takenouchi, M. T. Kamimura, T. C. Chen

    ANTICANCER RESEARCH   31 ( 4 )   1500 - 1501   2011.4

     More details

    Language:English   Publishing type:Research paper, summary (international conference)  

    Web of Science

    researchmap

  • 変異VDR(Arg274Leu)に対するセコステロイドリガンドの設計と合成(第329回会議研究発表要旨,脂溶性ビタミン総合研究委員会)

    本澤 忍, 高橋 尚志, 山本 康弘, 荒井 緑, 高野 真史, 澤田 大介, 山下 純, 杉浦 隆之, 橘高 敦史, 角田 真二, 齋藤 博, 高木 健一郎, 上村 みどり, 石塚 誠一, 竹之内 一弥, 榊 利之, 加藤 茂明, 栗原 正明

    ビタミン   85 ( 3 )   166 - 167   2011.3

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    DOI: 10.20632/vso.85.3_166_2

    CiNii Article

    researchmap

  • 2-II-20 2α位にアゾール環側鎖を有する活性型ビタミンD_3の合成と生物活性評価(一般演題要旨,日本ビタミン学会第63回大会講演要旨)

    高野 真史, 上村 みどり, 竹之 内一弥, 澤田 大介, 橘高 敦史, 松尾 実紀, 長谷川 麻美, 中村 優子, 齋藤 博, 角田 真二, 高木 健一郎, 落合 鋭士, 堀江 恭平

    ビタミン   85 ( 4 )   236 - 236   2011

     More details

    Language:Japanese   Publisher:公益社団法人 日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 1-I-6 新規15位置換活性型ビタミンD_3の合成研究(一般演題,日本ビタミン学会第62回大会発表要旨)

    熊谷 剛, 上村 みどり, 竹之内 一弥, 橘高 敦史, 澤田 大介, 新藤 香菜子, 高野 真史, 角田 真二, 齋藤 博, 高木 健一郎, 落合 鋭士, 堀江 恭平

    ビタミン   84 ( 4 )   2010

     More details

    Language:Japanese   Publisher:公益社団法人 日本ビタミン学会  

    CiNii Article

    researchmap

  • 1-I-5 14-epi-19-norprevitamin D_3から14-epi-19-nortachysterolへの展開(一般演題,日本ビタミン学会第62回大会発表要旨)

    澤田 大介, 佃 勇也, 堀江 恭平, 落合 鋭士, 齋藤 博, 角田 真二, 上村 みどり, 竹之内 一弥, 橘高 敦史

    ビタミン   84 ( 4 )   157 - 157   2010

     More details

    Language:Japanese   Publisher:公益社団法人 日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 1-I-7 2α位に2-(1H-テトラゾール-1-イル)エチル基及び 2-(2H-テトラゾール-2-イル)エチル基を有する活性型ビタミンD_3の合成と生物活性評価(一般演題,日本ビタミン学会第62回大会発表要旨)

    松尾 実紀, 上村 みどり, 竹之内 一弥, 澤田 大介, 橘高 敦史, 長谷川 麻美, 高野 真史, 中村 優子, 齋藤 博, 角田 真二, 高木 健一郎, 落合 鋭士, 堀江 恭平

    ビタミン   84 ( 4 )   158 - 158   2010

     More details

    Language:Japanese   Publisher:公益社団法人 日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 新規15位置換活性型ビタミンD3の合成とビタミンD受容体との相互作用および生物活性(第324回脂溶性ビタミン総合研究委員会研究発表要旨)

    新藤 香菜子, 高野 真史, 齋藤 望, 澤田 大介, 橘高 敦史, 角田 真二, 齋藤 博, 高木 健一郎, 上村 みどり, 石塚 誠一, 竹之内 一弥

    ビタミン   83 ( 10 )   593 - 593   2009.10

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    DOI: 10.20632/vso.83.10_593_1

    CiNii Article

    researchmap

  • 活性型ビタミンD3の2α位の構造修飾とVDRリガンド結合領域に存在する水分子(water channel)との相互作用と生物活性(第321回会議研究発表要旨,脂溶性ビタミン総合研究委員会)

    高野 真史, 澤田 大介, 橘高 敦史, 杉浦 隆之, 高木 健一郎, 石塚 誠一, 竹之内 一弥, 角田 真二, 上村 みどり, 林 恵子, 生城 真一, 榊 利之

    ビタミン   83 ( 5 )   328 - 329   2009.6

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    DOI: 10.20632/vso.83.5-6_328

    CiNii Article

    researchmap

  • 活性型ビタミンD3誘導体における核内受容体Water Channelの維持と生物活性(一般研究発表,日本ビタミン学会第61回大会研究発表要旨)

    高野 真史, 澤田 大介, 林 恵子, 生城 真一, 榊 利之, 角田 真二, 高木 健一郎, 堀江 恭平, 上村 みどり, 竹之内 一弥, 杉浦 隆之, 野尻 久雄, 橘高 敦史

    ビタミン   83 ( 4 )   206 - 206   2009.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • MEDI 428-New vitamin D3 analogs: 2alpha-(2,3-Dihydroxypropoxy)- and 2alpha-(2-hydroxypropoxy)- active vitamin D3 with highly potent VDR agonism

    Masashi Takano, Daisuke Sawada, Keiko Hayashi, Shin-ichi Ikushiro, Toshiyuki Sakaki, Ken-ichiro Takagi, Seiichi Ishizuka, Midori Takimoto-Kamimura, Maiko Gokoh, Takayuki Sugiura, Atsushi Kittaka

    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY   236   2008.8

     More details

    Language:English   Publishing type:Research paper, summary (international conference)  

    Web of Science

    researchmap

  • MEDI 87-Synthesis and biological evaluation of novel 2-substituted 14-epi-previtamin D3 analogs

    Daisuke Sawada, Yuya Tsukuda, Nozomi Saito, Tomoyuki Katayama, Hiroshi Saito, Ken-ichiro Takagi, Kazuya Takenouchi, Seiichi Ishizuka, Midori Takimoto-Kamimura, Masashi Takano, Atsushi Kittaka

    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY   236   2008.8

     More details

    Language:English   Publishing type:Research paper, summary (international conference)  

    Web of Science

    researchmap

  • 2位置換14-エピプレビタミンD3誘導体の合成と活性評価(一般研究発表,新世紀ビタミン学の展望と先進的展開を目指して,日本ビタミン学会第60回大会発表要旨)

    澤田 大介, 佃 勇也, 片山 智之, 齋藤 望, 齋藤 博, 竹之内 一弥, 高木 健一郎, 滑川 淳一, 石塚 誠一, 橘高 敦史

    ビタミン   82 ( 4 )   272 - 272   2008.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 14-エピプレビタミンD3への4位置換基の導入(一般研究発表,新世紀ビタミン学の展望と先進的展開を目指して,日本ビタミン学会第60回大会発表要旨)

    佃 勇也, 澤田 大介, 高木 健一郎, 石塚 誠一, 橘高 敦史

    ビタミン   82 ( 4 )   272 - 272   2008.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • 2α-(2-Hydroxypropoxy)-1α,25-dihydroxyvitamin D_3の合成と生物活性評価(一般研究発表,新世紀ビタミン学の展望と先進的展開を目指して,日本ビタミン学会第60回大会発表要旨)

    高野 真史, 澤田 大介, 林 恵子, 生城 真一, 榊 利之, 高木 健一郎, 石塚 誠一, 杉浦 隆之, 橘高 敦史

    ビタミン   82 ( 4 )   271 - 271   2008.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • Vitamin D hormone: Structural refinement of the seco-steroidal skeleton and the nuclear receptor mediated biological activity Reviewed

    Atsushi Kittaka, Daisuke Sawada, Masashi Takano, Nozomi Saito, Tomoyuki Katayama, Kanako Shindo, Yuya Tsukuda, Shinobu Honzawa, Midori A. Arai, Hiroshi Saito, Ken-ichiro Takagi, Kazuya Takenouchi, Seiichi Ishizuka, Toshiyuki Sakaki, Tai C. Chen

    ANTICANCER RESEARCH   28 ( 3A )   1618 - 1619   2008

     More details

    Language:English   Publishing type:Research paper, summary (international conference)  

    Web of Science

    researchmap

  • A環修飾14-epi-ビタミンD3と14-epi-19-ノルビタミンD3誘導体の合成と生物活性(第316回脂溶性ビタミン総合研究委員会発表要旨)

    澤田 大介, 齋藤 望, 片山 智之, 佃 勇也, 原 英己, 高野 真史, 橘高 敦史, 齋藤 博, 高木 健一郎, 千田 貴之, 原田 善史, 竹之内 一弥, 上村 みどり, 石塚 誠一, Chen Tai C

    ビタミン   81 ( 11 )   582 - 583   2007.11

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    DOI: 10.20632/vso.81.11_582

    CiNii Article

    researchmap

  • 2α-(2, 3-Dihydroxypropoxy)-1α,25-dihydroxyvitamin D3の合成と生物活性評価(ビタミン学の原点・栄養学への21世紀的回帰, 日本ビタミン学会第59回大会)

    高野 真史, 澤田 大介, 林 恵子, 生城 真一, 榊 利之, 高木 健一郎, 石塚 誠一, 岸本 成史, 杉浦 隆之, 橘高 敦史

    ビタミン   81 ( 4 )   151 - 151   2007.4

     More details

    Language:Japanese   Publisher:日本ビタミン学会  

    CiNii Article

    CiNii Books

    researchmap

  • A new and facile synthesis of carbamate- and urea-linked glycoconjugate using modified Curtius rearrangement Reviewed

    Daisuke Sawada, Shinya Sasayama, Hideyo Takahashi, Shiro Ikegami

    TETRAHEDRON LETTERS   47 ( 40 )   7219 - 7223   2006.10

  • Divergent synthesis of (L)-sugars and (L)-iminosugars from D-sugars Reviewed

    Hideyo Takahashi, Tomomi Shida, Yuko Hitomi, Yoshinori Iwai, Namisa Miyama, Kazusa Nishiyama, Daisuke Sawada, Shiro Ikegami

    CHEMISTRY-A EUROPEAN JOURNAL   12 ( 22 )   5868 - 5877   2006.7

  • Highly enantioselective cyanosilylation of aldehydes catalyzed by a Lewis acid-Lewis base bifunctional catalyst Reviewed

    Yoshitaka Hamashima, Daisuke Sawada, Hiroyuki Nogami, Motomu Kanai, Masakatsu Shibasaki

    Tetrahedron   57 ( 5 )   805 - 814   2001.1

▼display all

 

Class subject in charge

  • Frontier in Pharmaceutical Sciences (2024academic year) special  - その他

  • Overview of Drug Discovery and Drug Development (2024academic year) special  - その他

  • Medicinal Sciences (2024academic year) Second semester  - 金5~6

  • Medicinal Sciences (2024academic year) Third semester  - 金5~6

  • Experimental Organic Chemistry (2024academic year) 1st and 2nd semester  - その他5~9

  • Experimental Organic Chemistry (2024academic year) 1st and 2nd semester  - その他5~9

  • General Principles of the highest pharmacy study (2024academic year) special  - その他

  • Organic Chemistry and Natural Products Chemistry (2024academic year) special  - その他

  • Organic Chemistry and Natural Products Chemistry (2024academic year) special  - その他

  • Organic Chemistry 3 (2024academic year) Third semester  - 水1~2

  • Organic Chemistry 3 (2024academic year) Third semester  - 水1~2

  • Organic Chemistry 4 (2024academic year) Fourth semester  - 火5~7

  • Organic Chemistry 4 (2024academic year) Fourth semester  - 火5~7

  • Organic Chemistry B (2024academic year) 3rd and 4th semester  - [第3学期]水1~2, [第4学期]火5~7

  • Organic Chemistry B (2024academic year) 3rd and 4th semester  - [第3学期]水1~2, [第4学期]火5~7

  • Theory and Application of Organic Synthesis (2024academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2024academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2024academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2024academic year) Fourth semester  - 木5~6

  • Fine Organic Design (2024academic year) special  - その他

  • Seminar on Fine Organic Design (2024academic year) special  - その他

  • Fine Organic Design I (2024academic year) special  - その他

  • Fine Organic Design II (2024academic year) special  - その他

  • Fine Organic Synthesis (2024academic year) special  - その他

  • Practicals: Fine Organic Synthesis (2024academic year) special  - その他

  • Research Projects: Fine Organic Synthesis (2024academic year) special  - その他

  • Advanced Lectures: Fine Organic Synthesis (2024academic year) special  - その他

  • Practice in Fundamental Pharmaceutical Sciences II (2024academic year) 1st and 2nd semester  - その他5~9

  • Practice in Fundamental Pharmaceutical Sciences II (2024academic year) 1st and 2nd semester  - その他5~9

  • Frontier in Pharmaceutical Sciences (2023academic year) special  - その他

  • Overview of Drug Discovery and Drug Development (2023academic year) special  - その他

  • Medicinal Sciences (2023academic year) Second semester  - 金5~6

  • Medicinal Sciences (2023academic year) Third semester  - 金5~6

  • Experimental Organic Chemistry (2023academic year) 1st and 2nd semester  - その他5~9

  • Experimental Organic Chemistry (2023academic year) 1st and 2nd semester  - その他5~9

  • General Principles of the highest pharmacy study (2023academic year) special  - その他

  • Organic Chemistry and Natural Products Chemistry (2023academic year) special  - その他

  • Organic Chemistry and Natural Products Chemistry (2023academic year) special  - その他

  • Organic Chemistry 3 (2023academic year) Third semester  - 水1~2

  • Organic Chemistry 3 (2023academic year) Third semester  - 水1~2

  • Organic Chemistry 4 (2023academic year) Fourth semester  - 火5~7

  • Organic Chemistry 4 (2023academic year) Fourth semester  - 火5~7

  • Organic Chemistry B (2023academic year) 3rd and 4th semester  - [第3学期]水1~2, [第4学期]火5~7

  • Organic Chemistry B (2023academic year) 3rd and 4th semester  - [第3学期]水1~2, [第4学期]火5~7

  • Theory and Application of Organic Synthesis (2023academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2023academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2023academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2023academic year) Fourth semester  - 木5~6

  • Fine Organic Design (2023academic year) special  - その他

  • Seminar on Fine Organic Design (2023academic year) special  - その他

  • Fine Organic Design I (2023academic year) special  - その他

  • Fine Organic Design II (2023academic year) special  - その他

  • Fine Organic Synthesis (2023academic year) special  - その他

  • Practicals: Fine Organic Synthesis (2023academic year) special  - その他

  • Research Projects: Fine Organic Synthesis (2023academic year) special  - その他

  • Advanced Lectures: Fine Organic Synthesis (2023academic year) special  - その他

  • Practice in Fundamental Pharmaceutical Sciences II (2023academic year) 1st and 2nd semester  - その他5~9

  • Practice in Fundamental Pharmaceutical Sciences II (2023academic year) 1st and 2nd semester  - その他5~9

  • Seminar in Molecular Structure Analysis (2022academic year) Fourth semester  - 火3~4

  • Seminar in Molecular Structure Analysis (2022academic year) Fourth semester  - 火3~4

  • Medicinal Sciences (2022academic year) Second semester  - 金5~6

  • Medicinal Sciences (2022academic year) Third semester  - 金5~6

  • Organic Chemistry and Natural Products Chemistry (2022academic year) special  - その他

  • Organic Chemistry 3 (2022academic year) Third semester  - 水1~2

  • Organic Chemistry 3 (2022academic year) Third semester  - 水1~2

  • Organic Chemistry 4 (2022academic year) Fourth semester  - 水2~4

  • Organic Chemistry 4 (2022academic year) Fourth semester  - 水2~4

  • Organic Chemistry B (2022academic year) 3rd and 4th semester  - [第3学期]水1~2, [第4学期]水2~4

  • Organic Chemistry B (2022academic year) 3rd and 4th semester  - [第3学期]水1~2, [第4学期]水2~4

  • Theory and Application of Organic Synthesis (2022academic year) Fourth semester  - 木5~6

  • Theory and Application of Organic Synthesis (2022academic year) Fourth semester  - 木5~6

  • Fine Organic Design (2022academic year) special  - その他

  • Seminar on Fine Organic Design (2022academic year) special  - その他

  • Fine Organic Design I (2022academic year) special  - その他

  • Fine Organic Design II (2022academic year) special  - その他

  • Practice in Fundamental Pharmaceutical Sciences II (2022academic year) 1st and 2nd semester  - その他5~9

  • Practice in Fundamental Pharmaceutical Sciences II (2022academic year) 1st and 2nd semester  - その他5~9

  • Medicinal Sciences (2021academic year) Second semester  - 金5~6

  • Medicinal Sciences (2021academic year) Third semester  - 金5~6

  • Organic Chemistry and Natural Products Chemistry (2021academic year) Late  - その他

  • Organic Chemistry 3 (2021academic year) Third semester  - 水1,水2

  • Organic Chemistry 3 (2021academic year) Third semester  - 水1,水2

  • Organic Chemistry 4 (2021academic year) Fourth semester  - 水2,水3,水4

  • Organic Chemistry 4 (2021academic year) Fourth semester  - 水2,水3,水4

  • Organic Chemistry B (2021academic year) 3rd and 4th semester  - [第3学期]水1,水2, [第4学期]水2,水3,水4

  • Organic Chemistry B (2021academic year) 3rd and 4th semester  - [第3学期]水1,水2, [第4学期]水2,水3,水4

  • Organic Chemistry B (2021academic year) 3rd and 4th semester  - [第3学期]水1,水2, [第4学期]水2,水3,水4

  • Organic Chemistry B (2021academic year) 3rd and 4th semester  - [第3学期]水1,水2, [第4学期]水2,水3,水4

  • Theory and Application of Organic Synthesis (2021academic year) Fourth semester  - 木5,木6

  • Theory and Application of Organic Synthesis (2021academic year) Fourth semester  - 木5,木6

  • Fine Organic Design (2021academic year) special  - その他

  • Seminar on Fine Organic Design (2021academic year) special  - その他

  • Fine Organic Design I (2021academic year) special  - その他

  • Fine Organic Design II (2021academic year) special  - その他

  • Practice in Fundamental Pharmaceutical Sciences II (2021academic year) 1st and 2nd semester  - その他6~9

  • Practice in Fundamental Pharmaceutical Sciences II (2021academic year) 1st and 2nd semester  - その他6~9

  • Molecular Structure Analysis (2020academic year) 1st semester  - 月1,月2

  • Molecular Structure Analysis (2020academic year) 1st semester  - 月1,月2

  • Medicinal Sciences (2020academic year) Third semester  - 金5,金6

  • Structural Analysis of Medicine (2020academic year) 1st-4th semester  - [第1学期]月1,月2, [第2学期]その他, [第3学期]その他, [第4学期]火3,火4

  • Organic Chemistry and Natural Products Chemistry (2020academic year) special  - その他

  • Organic Chemistry 3 (2020academic year) Third semester  - 水1,水2

  • Organic Chemistry 3 (2020academic year) Third semester  - 水1,水2

  • Organic Chemistry 4 (2020academic year) Fourth semester  - 水3,水4

  • Organic Chemistry 4 (2020academic year) Fourth semester  - 水3,水4

  • Organic Chemistry III (2020academic year) 3rd and 4th semester  - 水1,水2

  • Theory and Application of Organic Synthesis (2020academic year) Fourth semester  - 木5,木6

  • Theory and Application of Organic Synthesis (2020academic year) Fourth semester  - 木5,木6

  • Fine Organic Design (2020academic year) special  - その他

  • Seminar on Fine Organic Design (2020academic year) special  - その他

  • Practice in Fundamental Pharmaceutical Sciences II (2020academic year) special  - その他

  • Practice in Fundamental Pharmaceutical Sciences II (2020academic year) special  - その他

▼display all