Article
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
Journal of medicinal chemistry - 26 Jun 2014
Rotili Dante, Tarantino Domenico, Nawrozkij Maxim B, Babushkin Alexandre S, Botta Giorgia, Marrocco Biagina, Cirilli Roberto, Menta Sergio, Badia Roger, Crespan Emmanuele, Ballante Flavio, Ragno Rino, Esté José A, Maga Giovanni, Mai Antonello
Abstract excerpt
A comparison of the effects of the 6-(2-chloro-6-fluorobenzyl)-2-(alkylthio)pyrimidin-4(3H)-ones (2-Cl-6-F-S-DABOs) 7-12 and the related 6-(2,6-difluorobenzyl) counterparts 13-15 in HIV-1 infected cells and in the HIV-1 reverse transcriptase (RT) assays is here described. The new 2-Cl-6-F-S-DABOs showed up to picomolar activity against wt HIV-1. Against clinically relevant HIV-1 mutants and in enzyme assays, the...
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