Issue 6, 2015

Identification of benzenesulfonamide quinoline derivatives as potent HIV-1 replication inhibitors targeting Rev protein

Abstract

Human immunodeficiency virus type 1 (HIV-1) Rev protein facilitates the export of viral RNA from nucleus to cytoplasm, which is a key step in HIV-1 pathogenesis and transmission. In this study, we have screened a commercial library and identified the hit compound 1 bearing a benzenesulfonamide quinoline scaffold that inhibited Rev activity and HIV-1 infectivity. Compounds bearing this scaffold were synthesized and their SAR was studied. We identified compound 20 with low toxicity and potent activity to inhibit HIV-1 replication by affecting Rev function.

Graphical abstract: Identification of benzenesulfonamide quinoline derivatives as potent HIV-1 replication inhibitors targeting Rev protein

Supplementary files

Article information

Article type
Paper
Submitted
22 Oct 2014
Accepted
19 Nov 2014
First published
19 Nov 2014

Org. Biomol. Chem., 2015,13, 1792-1799

Identification of benzenesulfonamide quinoline derivatives as potent HIV-1 replication inhibitors targeting Rev protein

F. Zhong, G. Geng, B. Chen, T. Pan, Q. Li, H. Zhang and C. Bai, Org. Biomol. Chem., 2015, 13, 1792 DOI: 10.1039/C4OB02247E

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