2. Academic Validation
  3. Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro

Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro

  • Bioorg Med Chem Lett. 2010 Jun 15;20(12):3534-6. doi: 10.1016/j.bmcl.2010.04.132.
Jun-Qiang Ran 1,  Ning Huang,  Hui Xu,  Liu-Meng Yang,  Min Lv,  Yong-Tang Zheng
Affiliations

Affiliation

  • 1 Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
PMID: 20488700 DOI: 10.1016/j.bmcl.2010.04.132
Abstract

In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC(50) values of 0.36 and 0.13 microg/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs.

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