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
Affiliations
- PMID: 26774579
- DOI: 10.1016/j.bmcl.2015.12.097
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Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity
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.
Copyright © 2015 Elsevier Ltd. All rights reserved.
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