Anti Human Immunodeficiency Virus-1 (HIV-1) Agents 3.  Synthesis and in Vitro Anti-HIV-1 Activity of Some N-Arylsulfonylindoles

Ling-Ling Fan; Wu-Qing Liu; Hui Xu; Liu-Meng Yang; Min Lv; Yong-Tang Zheng

doi:10.1248/cpb.57.797

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Anti Human Immunodeficiency Virus-1 (HIV-1) Agents 3. Synthesis and in Vitro Anti-HIV-1 Activity of Some N-Arylsulfonylindoles

Ling-Ling Fan, Wu-Qing Liu, Hui Xu, Liu-Meng Yang, Min Lv, Yong-Tang Zheng

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Keywords: N-arylsulfonylindole, human immunodeficiency virus type 1, inhibitor

JOURNAL FREE ACCESS

2009 Volume 57 Issue 8 Pages 797-800

DOI https://doi.org/10.1248/cpb.57.797

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Abstract

In order to find compounds with superior anti human immunodeficiency virus type 1 (HIV-1) activity, twelve simple N-arylsulfonylindoles (3a—l) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Several compounds demonstrated significant anti-HIV-1 activity, especially N-(3-nitrobenzene)sulfonyl-6-methylindole (3h) and N-(3-nitrobenzene)sulfonylindole (3i) showed the highest anti-HIV-1 activity with EC₅₀ values of 0.26 and 0.74 μg/ml, and TI values of 543.78 and >270.27, respectively.

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