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

• Main Authors: Xin Jin (Author), Shuai Wang (Author), Limin Zhao (Author), Wenjuan Huang (Author), Yinxiang Zhang (Author), Christophe Pannecouque (Author), Erik De Clercq (Author), Ge Meng (Author), Huri Piao (Author), Fener Chen (Author)
• Format: Book
• Published: Elsevier, 2023-03-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...