Optimization and biological evaluation of celastrol derivatives as Hsp90-Cdc37 interaction disruptors with improved druglike properties
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- 作者：Fen Jiang ; Hui-Jie Wang ; Qi-Chao Bao ; Lei Wang ; Yu-Hui Jin ; Qiong Zhang ; Di Jiang ; Qi-Dong You ; youqidong@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Xiao-Li Xu ; xuxiao_li@126.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Celastrol ; Hsp90&ndash ; Cdc37 interaction ; HTRF ; Structure&ndash ; activity relationship ; Druglike properties
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：1 November 2016
- 年：2016
- 卷：24
- 期：21
- 页码：5431-5439
- 全文大小：2982 K
文摘
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SAR study of celastrol derivatives as Hsp90–Cdc37 disruptors was elucidated.
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CEL20 showed improved Hsp90–Cdc37 disruption activity and in vitro antitumor activities.
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CEL20 possessed improved druglike properties.
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CEL20 induced clients degradation, cell cycle arrest and apoptosis in Panc-1 cells.