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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...
Autores principales: | Jin, Xin, Wang, Shuai, Zhao, Limin, Huang, Wenjuan, Zhang, Yinxiang, Pannecouque, Christophe, De Clercq, Erik, Meng, Ge, Piao, Huri, Chen, Fener |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2023
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Materias: | |
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 |
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