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题名: Design, Synthesis, and Biological Activities of Vibsanin B Derivatives: A New Class of HSP90 C-Terminal Inhibitors
作者: Shao, Li-Dong1; Su, Jia1; Ye, Baixin2, 3; Liu, Jiang-Xin1; Zuo, Zhi-Li1; Li, Yan1; Wang, Yue-Ying2, 3; Xia, Chengfeng1; Zhao, Qin-Shi1, 4
刊名: JOURNAL OF MEDICINAL CHEMISTRY
英文摘要: Previously, vibsanin B (ViB) was found to preferentially target HSP90 beta compared to HSP90 alpha. In this study, multiple experiments, including pull-down assays of biotin-ViB with recombinant HSP90 beta-NTD, MD, CTD, and full-length HSP90 beta, molecular docking of ViB and its derivatives to the HSP90 CTD, and a inhibition assay of interaction of the HSP90 beta CTD with GST-tagged cyclophilin 40 (Cyp40) by ViB derivatives, suggest that ViB can directly bind to the HSP90 C-terminus. On the basis of the docking predictions and primary structure-activity relationships (SARs), a series of ViB analogues devised with focus on the C18 position, along with compounds derivatized at the C4, C7, and C8 positions, were designed and chemically synthesized. Compound 12f (IC50 = 1.12 mu M against SK-BR-3) exhibits great potency with drug-like properties. Overall, our findings demonstrate that compounds with the vibsanin B scaffold are a new class of HSP90 C-terminal inhibitors with considerable potential as anticancer agents.
出版日期: 2017-11-09
卷号: 60, 期号:21, 页码:9053-9066
DOI标识: 10.1021/acs.jmedchem.7b01395
语种: 英语
ISSN号: 0022-2623
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/60372
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
2.Shanghai Jiao Tong Univ, Sch Med, RuiJin Hosp, State Key Lab Med Genom, Shanghai 200025, Peoples R China
3.Shanghai Jiao Tong Univ, Sch Med, RuiJin Hosp, Shanghai Inst Hematol, Shanghai 200025, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
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