Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs
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作为 HIV-1 NNRTI 的环烷基芳基嘧啶 (CAPY) 的设计、合成和生物学评价
DOI：
10.1016/j.bmc.2011.10.002
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发表时间：
2011-12-01
影响因子：
3.5
通讯作者：
Pannecouque, Christophe
中科院分区：
文献类型：
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作者：
Gu, Shuang-Xi;Yang, Shi-Qiong;Pannecouque, Christophe
以先导化合物二芳基嘧啶 (DAPY) 为基础设计了一系列 18 种环烷基芳基嘧啶 (CAPY)，合成并评估其体外抗 HIV 活性。其中，化合物1p对WT HIV-1表现出有效的抗HIV-1活性，EC50值为0.055 μM，选择性指数（SI）> 7290。还研究了这一系列新化合物的初步构效关系（SAR），丰富了二芳基嘧啶（DAPYs）的SAR。 (C) 2011 Elsevier Ltd. 保留所有权利。
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 mu M 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). (C) 2011 Elsevier Ltd. All rights reserved.