Synthesis and in vitro anti-HIV-1 activity of a series of N-arylsulfonyl-3-propionylindoles
2016 ◽
Vol 71
(5-6)
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pp. 105-109
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Keyword(s):
Anti Hiv
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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.
1998 ◽
Vol 9
(5)
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pp. 412-421
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2003 ◽
Vol 77
(7)
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pp. 4095-4103
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2001 ◽
Vol 45
(2)
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pp. 393-400
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1998 ◽
Vol 39
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pp. 101-111
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2002 ◽
Vol 76
(3)
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pp. 1015-1024
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2003 ◽
Vol 77
(1)
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pp. 291-300
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1998 ◽
Vol 72
(11)
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pp. 9337-9344
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2001 ◽
Vol 75
(8)
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pp. 3916-3924
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2000 ◽
Vol 74
(17)
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pp. 7699-7707
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