title: Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester.
abstract: A series of nitrogen-containing polyhydroxylated aromatics from caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase inhibitors. Most of these compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in the 3'-end processing and the strand transfer. Their key structure-activity relationship was also discussed.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province 250012, PR China.
authors.forename: Peng
authors.initials: P
authors.lastname: Wang
authors.forename: Chuan
authors.initials: C
authors.lastname: Liu
authors.forename: Tino
authors.initials: T
authors.lastname: Sanches
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhong
authors.forename: Bo
authors.initials: B
authors.lastname: Liu
authors.forename: Junlong
authors.initials: J
authors.lastname: Xiong
authors.forename: Nouri
authors.initials: N
authors.lastname: Neamati
authors.forename: Guisen
authors.initials: G
authors.lastname: Zhao
mesh_terms: D002109:Caffeic Acids / Q000737:chemistry*; D015195:Drug Design; D019427:HIV Integrase / Q000737:chemistry* / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009584:Nitrogen / Q000737:chemistry; D010626:Phenylethyl Alcohol / Q000031:analogs & derivatives* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D002109:Caffeic Acids; D019428:HIV Integrase Inhibitors; D019427:HIV Integrase; C055494:caffeic acid phenethyl ester; D010626:Phenylethyl Alcohol; D009584:Nitrogen; C514801:p31 integrase protein, Human immunodeficiency virus 1