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

Laboratory of Pharmaceutical Design & Synthesis, Department of Plant Protection, College of Forestry, Henan University of Science and Technology, Luoyang 471003, Henan, China
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Academic Editor: Jean Jacques Vanden Eynde
Pharmaceuticals 2015, 8(2), 221-229; https://doi.org/10.3390/ph8020221
Received: 9 April 2015 / Revised: 29 April 2015 / Accepted: 5 May 2015 / Published: 8 May 2015
Seven novel N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindole derivatives 4af 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. View Full-Text
Keywords: N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindoles; human immunodeficiency virus type-1; inhibitor N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindoles; human immunodeficiency virus type-1; inhibitor
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Che, Z.; Liu, S.; Tian, Y.; Hu, Z.; Chen, Y.; Chen, G. Design and Synthesis of Novel N-Arylsulfonyl-3-(2-yl-ethanone)-6-methylindole Derivatives as Inhibitors of HIV-1 Replication. Pharmaceuticals 2015, 8, 221-229.

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