Design, synthesis, and biological evaluation of bromophenol derivatives as protein tyrosine phosphatase 1B inhibitors

B Jiang, D Shi, Y Cui, S Guo

Index: Jiang, Bo; Shi, Dayong; Cui, Yongchao; Guo, Shuju Archiv der Pharmazie, 2012 , vol. 345, # 6 p. 444 - 453

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Citation Number: 11

Abstract

Abstract 3-Bromo-4, 5-bis (2, 3-dibromo-4, 5-dihydroxybenzyl)-1, 2-benzenediol (BDB) is a bromophenol purified from the marine red alga Rhodomela confervoides and exhibits potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC 50= 1.7 µmol/L). In an effort to improve the PTP1B inhibitory activity, a series of derivatives were designed, synthesized, and evaluated in vitro. The preliminary structure–activity relationship indicated that the ...