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

Fudi Zhong, Guannan Geng, Bing Chen, Ting Pan, Qianwen Li, Hui Zhang, Chuan Bai

Organic & biomolecular chemistry 2015 Feb 14

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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.

Citation

Fudi Zhong, Guannan Geng, Bing Chen, Ting Pan, Qianwen Li, Hui Zhang, Chuan Bai. Identification of benzenesulfonamide quinoline derivatives as potent HIV-1 replication inhibitors targeting Rev protein. Organic & biomolecular chemistry. 2015 Feb 14;13(6):1792-9