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

作者：Yu, Shenghui; Zhang, Linna; Yan, Shifeng; Wang, Peng; Sanchez, Tino; Christ, Frauke; Debyser, Zeger; Neamati, Nouri; Zhao, Guisen^*

来源：Journal of Enzyme Inhibition and Medicinal Chemistry, 2012, 27(5): 628-640.

DOI：10.3109/14756366.2011.604851

• HIV-1
• integrase inhibitors
• polyhydroxylated aromatics
• structure-activity relationship

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 mu M against strand transfer reaction. Their key structure-activity relationships were also discussed.

• 出版日期2012-10
• 单位山东大学; KU Leuven