Design, Synthesis and Structure-activity Studies of Rhodanine Derivatives as HIV-1 Integrase Inhibitors
AbstractRaltegravir 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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Ramkumar, K.; Yarovenko, V.N.; Nikitina, A.S.; Zavarzin, I.V.; Krayushkin, M.M.; Kovalenko, L.V.; Esqueda, A.; Odde, S.; Neamati, N. Design, Synthesis and Structure-activity Studies of Rhodanine Derivatives as HIV-1 Integrase Inhibitors. Molecules 2010, 15, 3958-3992.
Ramkumar K, Yarovenko VN, Nikitina AS, Zavarzin IV, Krayushkin MM, Kovalenko LV, Esqueda A, Odde S, Neamati N. Design, Synthesis and Structure-activity Studies of Rhodanine Derivatives as HIV-1 Integrase Inhibitors. Molecules. 2010; 15(6):3958-3992.Chicago/Turabian Style
Ramkumar, Kavya; Yarovenko, Vladimir N.; Nikitina, Alexandra S.; Zavarzin, Igor V.; Krayushkin, Mikhail M.; Kovalenko, Leonid V.; Esqueda, Adrian; Odde, Srinivas; Neamati, Nouri. 2010. "Design, Synthesis and Structure-activity Studies of Rhodanine Derivatives as HIV-1 Integrase Inhibitors." Molecules 15, no. 6: 3958-3992.