Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: Boosting the safety and metabolic stability

Development of fluorine-substituted NH2-biphenyl-diarylpyrimidines as highly potent non-nucleoside reverse transcriptase inhibitors: Boosting the safety and metabolic stability

Our recent studies for nonnucleoside reverse transcriptase inhibitors identified a highly potent compound JK-4b against WT HIV-1 (EC50 = 1.0 nmol/L), but the poor metabolic stability in human liver microsomes (t1/2 = 14.6 min) and insufficient selectivity (SI = 2059) with high cytotoxicity (CC50 = 2...

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Bibliographic Details
Main Authors: Xin Jin, Shuai Wang, Limin Zhao, Wenjuan Huang, Yinxiang Zhang, Christophe Pannecouque, Erik De Clercq, Ge Meng, Huri Piao, Fener Chen
Format: Article
Language:English
Published: Elsevier 2023-03-01
Series:Acta Pharmaceutica Sinica B
Subjects:
HIV-1
NNRTI
DAPYs
Safety
Metabolic stability
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383522003677

Internet

http://www.sciencedirect.com/science/article/pii/S2211383522003677

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