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ID: ALA4428129

Journal: Bioorg Med Chem

Title: Analysis of quinolinequinone reactivity, cytotoxicity, and anti-HIV-1 properties.

Authors: Alfadhli A, Mack A, Harper L, Berk S, Ritchie C, Barklis E.

Abstract: We have analyzed a set of quinolinequinones with respect to their reactivities, cytotoxicities, and anti-HIV-1 properties. Most of the quinolinequinones were reactive with glutathione, and several acted as sulfhydryl crosslinking agents. Quinolinequinones inhibited binding of the HIV-1 matrix protein to RNA to varying degrees, and several quinolinequinones showed the capacity to crosslink HIV-1 matrix proteins in vitro, and HIV-1 structural proteins in virus particles. Cytotoxicity assays yielded quinolinequinone CC50 values in the low micromolar range, reducing the potential therapeutic value of these compounds. However, one compound, 6,7-dichloro-5,8-quinolinequinone potently inactivated HIV-1, suggesting that quinolinequinones may prove useful in the preparation of inactivated virus vaccines or for other virucidal purposes.

CiteXplore: 27663546

DOI: 10.1016/j.bmc.2016.09.028