Lu Huan-Huan, Xue Ping, Zhu Yuan-Yuan, Ju Xiu-Lian, Zheng Xiao-Jiao, Zhang Xun, Xiao Ting, Pannecouque Christophe, Li Ting-Ting, Gu Shuang-Xi
Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering & Pharmacy, Wuhan Institute of Technology, Wuhan 430205, China.
School of Chemistry and Environmental Engineering, Wuhan Institute of Technology, Wuhan 430205, China.
Bioorg Med Chem. 2017 Apr 15;25(8):2491-2497. doi: 10.1016/j.bmc.2017.03.009. Epub 2017 Mar 6.
30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs. The anti-HIV-1 activities of all target molecules were evaluated, and most of them exhibited potent anti-HIV-1 (WT) activities and low cytotoxicities. Among which, compound 4g showed excellent activities against WT HIV-1 with an EC value of 5.8nM and SI of up to 26,034. Another compound 4ab bearing a novel pyridinyl Wing α also displayed attractive activities. The structure-activity relationship (SAR) study was also summarized.
合成了30种新型二芳基嘧啶类似物用于进一步的结构修饰，不仅涉及连接基团，还包括二芳基嘧啶的翼α部分。评估了所有目标分子的抗HIV-1活性，其中大多数表现出强效的抗HIV-1（野生型）活性和低细胞毒性。其中，化合物4g对野生型HIV-1表现出优异的活性，EC值为5.8nM，SI高达26,034。另一种带有新型吡啶基翼α的化合物4ab也显示出有吸引力的活性。还总结了构效关系（SAR）研究。
