Development of fluorine-substituted NH(2)-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 (EC(50) = 1.0 nmol/L), but the poor metabolic stability in human liver microsomes (t(1/2) = 14.6 min) and insufficient selectivity (SI = 2059) with high cytotoxicity (CC(5...

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Detalles Bibliográficos
Autores principales: Jin, Xin, Wang, Shuai, Zhao, Limin, Huang, Wenjuan, Zhang, Yinxiang, Pannecouque, Christophe, De Clercq, Erik, Meng, Ge, Piao, Huri, Chen, Fener
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2023
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10031149/
https://www.ncbi.nlm.nih.gov/pubmed/36970200
http://dx.doi.org/10.1016/j.apsb.2022.08.017

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10031149/
https://www.ncbi.nlm.nih.gov/pubmed/36970200
http://dx.doi.org/10.1016/j.apsb.2022.08.017

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