Synthesis, structure–activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors
…, X Zhang, SQ Yang, LM Yang, SX Gu, YT Zheng…
Index: Ma, Xiao-Dong; He, Qiu-Qin; Zhang, Xuan; Yang, Shi-Qiong; Yang, Liu-Meng; Gu, Shuang-Xi; Zheng, Yong-Tang; Chen, Fen-Er; Dai, Hui-Fang European Journal of Medicinal Chemistry, 2012 , vol. 58, p. 504 - 512
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Citation Number: 5
Abstract
A series of N-phenylarylformamide derivatives (PAFAs) with anti-wild-type HIV-1 activity (EC50 values) ranging from 0.3 nM to 5.1 nM and therapeutic index (TI) ranging from 10 616 to 271 000 were identified as novel non-nucleoside reverse transcriptase inhibitors. Among them, compound 13g (EC50= 0.30 nM, TI= 184 578), 13l (EC50= 0.37 nM, TI= 212 819), 13m (EC50= 0.32 nM, TI= 260 617) and 13r (EC50= 0.27 nM, TI= 271 000) displayed the ...
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