title: 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.
authors.affiliation: Institute of Human Virology, Key Laboratory of Tropical Diseases Control of Ministry of Education of China, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, 510080, China. zhangh92@mail.sysu.edu.cn baichuan@mail.sysu.edu.cn.
authors.forename: Fudi
authors.initials: F
authors.lastname: Zhong
authors.forename: Guannan
authors.initials: G
authors.lastname: Geng
authors.forename: Bing
authors.initials: B
authors.lastname: Chen
authors.forename: Ting
authors.initials: T
authors.lastname: Pan
authors.forename: Qianwen
authors.initials: Q
authors.lastname: Li
authors.forename: Hui
authors.initials: H
authors.lastname: Zhang
authors.forename: Chuan
authors.initials: C
authors.lastname: Bai
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001555:Benzene Derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015694:Gene Products, rev / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D019380:Anti-HIV Agents; D001555:Benzene Derivatives; D015694:Gene Products, rev; D011804:Quinolines; D013449:Sulfonamides