Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs

…, E De Clercq, J Balzarini, C Pannecouque

Index: Gu, Shuang-Xi; Yang, Shi-Qiong; He, Qiu-Qin; Ma, Xiao-Dong; Chen, Fen-Er; Dai, Hui-Fang; Clercq, Erik De; Balzarini, Jan; Pannecouque, Christophe Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 23 p. 7093 - 7099

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Citation Number: 9

Abstract

A series of 18 cycloalkyl arylpyrimidines (CAPYs) were designed from lead compounds diarylpyrimidines (DAPYs), synthesized and evaluated for in vitro anti-HIV activity. Among them, the compound 1p displayed potent anti-HIV-1 activity against WT HIV-1 with an EC50 value of 0.055 μM and a selectivity index (SI)> 7290. The preliminary structure–activity relationship (SAR) of this new series of compounds was also investigated, which enriched ...

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