The first synthesis of natural disulfide bruguiesulfurol and biological evaluation of its derivatives as a novel scaffold for PTP1B inhibitors.
Basic Information
ID: ALA2417434
Journal: Bioorg Med Chem Lett
Title: The first synthesis of natural disulfide bruguiesulfurol and biological evaluation of its derivatives as a novel scaffold for PTP1B inhibitors.
Authors: Chen J, Jiang CS, Ma WQ, Gao LX, Gong JX, Li JY, Li J, Guo YW.
Abstract: Bruguiesulfurol (1), a cyclic 4-hydroxy-dithiosulfonate isolated from mangrove plant Bruguiera gymnorrhiza, was concisely synthesized for the first time in four steps, and a series of its synthetic derivatives were evaluated for in vitro inhibitory effects on PTP1B and related PTPs. Some derivatives were found to have improved pharmacological profile compared with hit 1. Among them, 5a showed the potent selectivity towards PTP1B over other PTPs, including TCPTP, and 7j exhibited the strongest PTP1B inhibitory activity with an IC50 value of 4.54 μM.
CiteXplore: 23942421
DOI: 10.1016/j.bmcl.2013.07.039
Patent ID: ┄