1350435-20-9Relevant academic research and scientific papers
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs
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
, p. 7093 - 7099 (2011)
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 the SAR of diarylpyrimidines (DAPYs).
