title: Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro.
abstract: A variety of N-acetyl-beta-aryl-1,2-didehydroethylamines were synthesized by direct reduction-acetylation of beta-aryl-nitroolefins and assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of >13.2 with CC50 value of >0.787 mM in C8166 cells. This structure-activity relationship (SAR) study provided a new lead for design and discovery of more potent and selective analogues act as NNRTIs.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming, Yunnan 650204, PR China.
authors.forename: Pi
authors.initials: P
authors.lastname: Cheng
authors.forename: Zhi-Yong
authors.initials: ZY
authors.lastname: Jiang
authors.forename: Rui-Rui
authors.initials: RR
authors.lastname: Wang
authors.forename: Xue-Mei
authors.initials: XM
authors.lastname: Zhang
authors.forename: Qian
authors.initials: Q
authors.lastname: Wang
authors.forename: Yong-Tang
authors.initials: YT
authors.lastname: Zheng
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.forename: Ji-Jun
authors.initials: JJ
authors.lastname: Chen
mesh_terms: D005021:Ethylamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000201:enzymology*; D015394:Molecular Structure; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D005021:Ethylamines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase