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Design and Synthesis of Novel N-Arylsulfonyl-3-(2-yl-ethanone)-6-methylindole Derivatives as Inhibitors of HIV-1 Replication.

Authors
  • Che, Zhiping
  • Liu, Shengming
  • Tian, Yuee
  • Hu, Zhenjie
  • Chen, Yingwu
  • Chen, Genqiang
Type
Published Article
Journal
Pharmaceuticals
Publisher
MDPI AG
Publication Date
Jan 01, 2015
Volume
8
Issue
2
Pages
221–229
Identifiers
DOI: 10.3390/ph8020221
PMID: 26110320
Source
Medline
Keywords
License
Unknown

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.

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