Synthesis, anti-HIV-1 integrase, and cytotoxic activities of 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives

Several 4-chloro-N-(4-oxopyrimidin-2-yl)-2-mercaptobenzenesulfonamide derivatives 13–28 and 35–44 have been synthesized and tested as potential HIV-1 integrase (IN) inhibitors. Compounds 15–17, 19, 21–28, 36 and 41 inhibited IN with IC50 values in the range of 3.3–63.0 μM. The compounds 13, 15, 16, 21–24 and 26–28 were further tested at the US National Cancer Institute for their in vitro activity against a panel of 53–57 human tumor cell lines. The compounds 26–28 were inactive, whereas the other compounds exhibited high or reasonable activity (GI50 < 0.01–20.0 μM) against one or more human tumor cell lines.

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