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Elsevier, Bioorganic and Medicinal Chemistry, 23(19), p. 7093-7099

DOI: 10.1016/j.bmc.2011.10.002

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

Journal article published in 2011 by Shuang-Xi Gu, Shi-Qiong Yang, Qiu-Qin He, Xiao-Dong Ma, Xiao-Dong, Fen-Er Chen, Hui-Fang Dai, Erik De Clercq, Erik De Clercq, Jan Balzarini, Christophe Pannecouque
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This paper is available in a repository.

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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 EC(50) 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 the SAR of diarylpyrimidines (DAPYs).