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

被引：45

作者：

Zhang, Li ^{[1
]}

Jiang, Cheng-Shi ^{[1
,2
]}

Gao, Li-Xin ^{[1
]}

Gong, Jing-Xu ^{[1
]}

Wang, Zhong-Hua ^{[3
]}

Li, Jing-Ya ^{[1
]}

Li, Jia ^{[1
]}

Li, Xu-Wen ^{[1
]}

Guo, Yue-Wei ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China

[2] Univ Jinan, Sch Biol Sci & Technol, 336 Nan Xin Zhuang Xi Rd, Jinan 250022, Shandong, Peoples R China

[3] Shanghai Inst Technol, Sch Chem & Environm Engn, 100 Hai Quan Rd, Shanghai 201418, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 03期

关键词：

Phidianidine; Oxadiazole derivative; PTP1B inhibitor; Specific selectivity; Docking analysis; Function-oriented synthesis; PROTEIN-TYROSINE-PHOSPHATASE; BIOLOGICAL EVALUATION; INSULIN SENSITIVITY; INDOLE ALKALOIDS; 1B INHIBITORS; RESISTANCE; MICE;

D O I：

10.1016/j.bmcl.2015.12.097

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：778 / 781

页数：4

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