Art

J-GLOBAL ID：202002232750181809   Reference number：20A1132070

Design, Synthesis, and Conformation-Activity Study of Unnatural Bridged Bicyclic Depsipeptides as Highly Potent Hypoxia Inducible Factor-1 Inhibitors and Antitumor Agents

非常に強力な低酸素誘導因子-1阻害剤および抗腫瘍薬としての非天然架橋二環デプシペプチドの設計,合成および立体配座活性研究【JST・京大機械翻訳】

Author (7)： Koike Kota (Laboratory of Pharmaceutical and Medicinal Chemistry, Gifu Pharmaceutical University, Gifu, Japan) ,  Nagano Masanobu (Department of Chemistry, The University of Tokyo, Japan) ,  Ebihara Masahiro (Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University, Gifu, Japan) ,  Hirayama Tasuku (Laboratory of Pharmaceutical and Medicinal Chemistry, Gifu Pharmaceutical University, Gifu, Japan) ,  Tsuji Mieko (Laboratory of Pharmaceutical and Medicinal Chemistry, Gifu Pharmaceutical University, Gifu, Japan) ,  Suga Hiroaki (Department of Chemistry, The University of Tokyo, Japan) ,  Nagasawa Hideko (Laboratory of Pharmaceutical and Medicinal Chemistry, Gifu Pharmaceutical University, Gifu, Japan)
Material： Journal of Medicinal Chemistry  (J Med Chem)
Volume： 63  Issue： 8  Page： 4022-4046  Publication year： 2020 
JST Material Number： D0102A  ISSN： 0022-2623  CODEN： JMCMAR  Document type： Article
Article type： 原著論文  Country of issue： United States (USA)  Language： ENGLISH (EN)

Abstract/Point： By carrying out structural mod...

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Thesaurus term： *steric conformation ,  *peptide ,  *antitumor drug ,  *tumor ,  *oxygen deficiency ,  biological activity ,  *depsipeptide ,  cytotoxicity ,  robustness ,  Cell Line ,  molecular modeling ,  Transcriptional Activation ,  protein expression ,  conformational search ,  cyclopeptide ,  oligopeptide

JST classification (3)： Enzyme in general  (EB09010D) ,  Basic research of enzyme preparations and enzyme inhibitor preparations  (GW21010W) ,  Structure-activity relationship of drugs  (GV01050B)

Substance index (1)： Echinomycin

Terms in the title (10)： 低酸素誘導因子 ,  阻害剤 ,  抗腫瘍薬 ,  架橋 ,  二環 ,  デプシペプチド ,  設計 ,  立体配座 ,  活性 ,  研究