Synthesis of a series of novel 2, 4, 5-trisubstituted selenazole compounds as potential PLTP inhibitors

C Ling, Z Zheng, XC Jiang, W Zhong, S Li

Index: Ling, Cui; Zheng, Zhibing; Jiang, Xian Cheng; Zhong, Wu; Li, Song Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 5123 - 5125

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Citation Number: 14

Abstract

Based on a homology-modeled structure of PLTP and characteristic structural features of reported cholesteryl ester transfer protein (CETP) inhibitors, we designed and synthesized a novel series of 2, 4, 5-trisubstituted selenazole compounds. Biological evaluation reveals that compounds 12 and 17 exhibit favorable PLTP activity, and their IC50s are 8μM and 10μM, respectively.