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. 2016 Feb 1;26(3):778-781.
doi: 10.1016/j.bmcl.2015.12.097. Epub 2015 Dec 29.

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

Li Zhang  1 , Cheng-Shi Jiang  2 , Li-Xin Gao  1 , Jing-Xu Gong  1 , Zhong-Hua Wang  3 , Jing-Ya Li  1 , Jia Li  1 , Xu-Wen Li  4 , Yue-Wei Guo  5
Affiliations

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

Li Zhang et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: Docking analysis; Function-oriented synthesis; Oxadiazole derivative; PTP1B inhibitor; Phidianidine; Specific selectivity.

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