Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity

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• 作者：Li Zhang^a ; ^&dagger ; ; Cheng-Shi Jiang^a ; ^b ; ^&dagger ; ; Li-Xin Gao^a ; Jing-Xu Gong^a ; Zhong-Hua Wang^c ; Jing-Ya Li^a ; Jia Li^a ; Xu-Wen Li^a ; ^{xwli@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author} ; Yue-Wei Guo^a ; ^{ywguo@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Phidianidine ; Oxadiazole derivative ; PTP1B inhibitor ; Specific selectivity ; Docking analysis ; Function-oriented synthesis
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：26
• 期：3
• 页码：778-781
• 全文大小：2477 K

文摘

A series of phidianidine B derivatives were synthesized by introducing various heterocyclic rings. Their inhibitory effects on PTP1B and other PTPs (TCPTP, SHP1, SHP2 and LAR) were evaluated. A majority of them displayed significant inhibitory potency and specific selectivity over PTP1B. The SAR and molecular docking analysis were also described.