Structural modification of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors

• 作 者: Zi-Hong Yan Hai-Qiu Wu Qiu-Qin He Fen-Er Chen Erik De Clercq Jan Balzarini Christophe Pannecouque
• 机 构: Department of Chemistry,Fudan University,220 Handan Road,Shanghai 200433 P.R.China
• 出 处: 全国药物化学学术会议暨第四届中英药物化学学术会议
• 发表日期: 2013年11期
• 关键词: HIV-1 RT NNRTIs DAPYs QSAR

　　A series of novel diarylpyrimidine with a halogen substituent on the methylene linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell culture.Most of these target compounds displayed anti-HIV-1 activity with micromolar to nanomolar EC50 values.