title: Synthesis and in vitro anti-HIV-1 activity of a series of N-arylsulfonyl-3-propionylindoles.
abstract: Fifteen N-arylsulfonyl-3-propionylindoles (3a-o) were prepared and preliminarily evaluated as in vitro inhibitors of human immunodeficiency virus type-1 (HIV-1). Three compounds 3c, 3g and 3i exhibited potent anti-HIV-1 activity with effective concentration (EC(50)) values of 0.8, 4.0 and 1.2 μg/mL, and therapeutic index (TI) values of 11.7, 16.6 and 84.1, respectively. N-(m-Nitro)phenylsulfonyl-3-propionyl-6-methylindole (3i) exhibited the most promising and best activity against HIV-1 replication. The cytotoxicity of these compounds was assessed as well.
authors.forename: Zhiping
authors.initials: Z
authors.lastname: Che
authors.forename: Yuee
authors.initials: Y
authors.lastname: Tian
authors.forename: Zhenjie
authors.initials: Z
authors.lastname: Hu
authors.forename: Yingwu
authors.initials: Y
authors.lastname: Chen
authors.forename: Shengming
authors.initials: S
authors.lastname: Liu
authors.forename: Genqiang
authors.initials: G
authors.lastname: Chen
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D015658:HIV Infections / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D015497:HIV-1 / Q000502:physiology*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D019380:Anti-HIV Agents; D007211:Indoles