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- Title
Design and Synthesis of Novel N-Arylsulfonyl-3-(2-yl-ethanone)-6-methylindole Derivatives as Inhibitors of HIV-1 Replication.
- Authors
Zhiping Che; Shengming Liu; Yuee Tian; Zhenjie Hu; Yingwu Chen; Genqiang Chen
- Abstract
Seven novel N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindole derivatives 4a-f and 6 were readily synthesized and have been identified as inhibitors of human immunodeficiency virus type-1 (HIV-1) replication. Initial biological studies indicated that among these derivatives, N-(p-ethyl)phenylsulfonyl-3-[2-morpholinoethanone]-6-methylindole (4f) and N-(p-ethyl)phenylsulfonyl-3-[2-(5-phenyl-1,3,4-oxadiazole-2-yl-thio)ethanone]-6- methylindole (6) showed the most promising activity against HIV-1 replication. The effective concentration (EC50) and therapeutic index (TI) values of 4f and 6 were 9.42/4.62 μM, and >49.77/66.95, respectively. The cytotoxicity of these compounds has also been assessed. No significant cytotoxicities were found for any of these compounds.
- Subjects
CHEMICAL synthesis; HIV fusion inhibitors; AIDS; DRUG efficacy; THERAPEUTICS; HIV infections; DRUG therapy
- Publication
Pharmaceuticals (14248247), 2015, Vol 8, Issue 2, p221
- ISSN
1424-8247
- Publication type
Article
- DOI
10.3390/ph8020221