Raltegravir was the first HIV-1 integrase inhibitor that gained FDA approval for use in the treatment of HIV-1 infection. Because of the emergence of IN inhibitor-resistant viral strains, there is a need to identify innovative second-generation IN inhibitors. Previously, we identified 2-thioxo-4-thiazolidinone (rhodanine)-containing compounds as IN inhibitors. Herein, we report the design, synthesis and docking studies of a series of novel rhodanine derivatives as IN inhibitors. All these compounds were further tested against human apurinic/apyrimidinic endonuclease 1 (APE1) to determine their selectivity. Two compounds showed significant cytotoxicity in a panel of human cancer cell lines. Taken together, our results show that rhodanines are a promising class of compounds for developing drugs with antiviral and anticancer properties.

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A series of new 2 thioxo 1,3 thiazolidin 4 one derivatives containing arylidene, arylazo, and aminomethylene fragments in position 5 of the rhodanine cycle was synthesized.

Thiazole derivatives R 0260Synthesis of 2-Thioxo-1,3-thiazolidin-4-one Derivatives. -36 Members of the title series are prepared. -(YAROVENKO*, V. N.; NIKITINA, A. S.; ZAVARZIN, I. V.; KRAYUSHKIN, M. M.; KOVALENKO, L. V.; Russ.