Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold

…, XK Guo, F Jiang, B Cherfaoui, HP Sun, QD You

Index: Jia, Jian-Min; Liu, Fang; Xu, Xiao-Li; Guo, Xiao-Ke; Jiang, Fen; Cherfaoui, Bahidja; Sun, Hao-Peng; You, Qi-Dong Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 6 p. 1557 - 1561

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Citation Number: 3

Abstract

Abstract Previously, we identified 1-(2-(4-bromophenoxy) ethoxy)-3-(4-(2-methoxyphenyl) piperazin-1-yl) propan-2-ol (1) as a novel Hsp90 inhibitor with moderate activity through virtual screening. In this study, we report the optimization process of 1. A series of analogues containing the 1-phenylpiperazine core scaffold were synthesized and evaluated. The structure–activity relationships (SAR) for these compounds was also discussed for further ...