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Paper | Regular issue | Vol 85, No. 8, 2012, pp.1897-1911
Published online, 18th June, 2012
DOI: 10.3987/COM-12-12477
Design, Synthesis and Biological Activity Evaluation of 2-Mercapto-4(3H)-quinazolinone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B

Hui Li, Jin-Ping Wang, Fan Yang, Ting Liu, Wen-Wei Qiu, Jing-Ya Li, Jia Li,* and Jie Tang*

*Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, China

Abstract

A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC50 = 1.50 μg/mL), and 27 possessed the best selectivity of 3.0-fold.