Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity

…, P Wang, T Sanchez, F Christ, Z Debyser…

文献索引：Yu, Shenghui; Zhang, Linna; Yan, Shifeng; Wang, Peng; Sanchez, Tino; Christ, Frauke; Debyser, Zeger; Neamati, Nouri; Zhao, Guisen Journal of Enzyme Inhibition and Medicinal Chemistry, 2012 , vol. 27, # 5 p. 628 - 640

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被引用次数: 5

摘要

Four series of forty-five nitrogen-containing polyhydroxylated aromatics based on caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase (IN) inhibitors. Most of these compounds inhibited IN catalytic activities in low micromolar range. Among these new analogues, compounds 9e and 9f were the most potent IN inhibitors with IC50 value of 0.7 μM against strand transfer reaction. Their key structure-activity relationships were also ...