Synthesis and HIV-1 Integrase Inhibition Activity of some N-Arylindoles

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

doi:10.1248/cpb.56.720

Notes

Synthesis and HIV-1 Integrase Inhibition Activity of some N-Arylindoles

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

Author information

Hui Xu
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University
Wu-Qing Liu
Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences
Ling-Ling Fan
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University
Yang Chen
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University
Liu-Meng Yang
Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences
Lei Lv
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University
Yong-Tang Zheng
Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences

Keywords: N-arylindole, anti-human immunodeficiency virus type 1, integrase inhibitor, synthesis

JOURNAL FREE ACCESS

2008 Volume 56 Issue 5 Pages 720-722

DOI https://doi.org/10.1248/cpb.56.720

Details

Abstract

Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC₅₀ value of 7.88 μg/ml and TI value of 24.61. Meantime, some structure–activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors.

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