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Synthesis and in vitro anti-HIV-1 activity of a series of N-arylsulfonyl-3-propionylindoles

Authors
  • Che, Zhiping
  • Tian, Yuee
  • Hu, Zhenjie
  • Chen, Yingwu
  • Liu, Shengming
  • Chen, Genqiang
Type
Published Article
Journal
Zeitschrift für Naturforschung C
Publisher
Walter de Gruyter GmbH
Publication Date
Apr 28, 2016
Volume
71
Issue
5-6
Pages
105–109
Identifiers
DOI: 10.1515/znc-2015-0122
Source
De Gruyter
Keywords
License
Yellow

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 (EC50) 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.

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