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Design, Synthesis and Structure-activity Studies of Rhodanine Derivatives as HIV-1 Integrase Inhibitors

Author(s): Kavya Ramkumar | Vladimir N. Yarovenko | Alexandra S. Nikitina | Igor V. Zavarzin | Mikhail M. Krayushkin | Leonid V. Kovalenko | Adrian Esqueda | Srinivas Odde | Nouri Neamati

Journal: Molecules
ISSN 1420-3049

Volume: 15;
Issue: 6;
Start page: 3958;
Date: 2010;
Original page

Keywords: rhodanine | HIV-1 | integrase | APE1 | 2-thioxo-4-thiazolidinone | docking

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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