Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity. Issue 3 (1st February 2016)

• Record Type: Journal Article
• Authors: Zhang, Li; Jiang, Cheng-Shi; Gao, Li-Xin; Gong, Jing-Xu; Wang, Zhong-Hua; Li, Jing-Ya; Li, Jia; Li, Xu-Wen; Guo, Yue-Wei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 3(2016)
• Page Start: 778
• Page End: 781
• Publication Date: 2016-02-01
• Subjects: Phidianidine -- Oxadiazole derivative -- PTP1B inhibitor -- Specific selectivity -- Docking analysis -- Function-oriented synthesis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.12.097
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Function-oriented synthesis of phidianidine B derivatives was accomplished, their specific inhibitory effects on PTP1B, the SAR and molecular docking analysis were described. 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.