具有强效抗HIV-1活性的二氮杂萘酮（DAPY）类似物的结构修饰
Structural modifications of DAPY analogues with potent anti-HIV-1 activity.
作者信息
Feng Xiao-Qing, Liang Yong-Hong, Zeng Zhao-Sen, Chen Fen-Er, Balzarini Jan, Pannecouque Christophe, De Clercq Erik
机构信息
Department of Chemistry, Fudan University, Shanghai, P.R. China.
出版信息
ChemMedChem. 2009 Feb;4(2):219-24. doi: 10.1002/cmdc.200800334.
A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were designed, with all compounds exhibiting strong activity against wild-type HIV-1.A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were synthesized and evaluated for their in vitro activity against HIV in MT-4 cells. All compounds exhibited strong activity against wild-type HIV-1. The most active compound showed activity against wild-type HIV-1 with an EC(50) value of 2.35 nM and against the double mutant strain (K103N+Y181C) with an EC(50) value of 6.6 microM, with a selectivity index greater than 60 000 against wild-type HIV-1. Additionally, some compounds also showed activity against HIV-2 (EC(50)=5.82 microM).
设计了一系列新型的在C4位带有萘基部分的二芳基嘧啶类似物（DAPYs），所有化合物对野生型HIV-1均表现出强效活性。合成了一系列新型的在C4位带有萘基部分的二芳基嘧啶类似物（DAPYs），并在MT-4细胞中评估了它们对HIV的体外活性。所有化合物对野生型HIV-1均表现出强效活性。活性最强的化合物对野生型HIV-1的EC(50)值为2.35 nM，对双突变株（K103N+Y181C）的EC(50)值为6.6 microM，对野生型HIV-1的选择性指数大于60000。此外，一些化合物对HIV-2也表现出活性（EC(50)=5.82 microM）。
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