Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors

R Puig-de-la-Bellacasa, L Giménez…

Index: Puig-De-La-Bellacasa, Raimon; Gimenez, Laura; Pettersson, Sofia; Pascual, Rosalia; Gonzalo, Encarna; Este, Jose A.; Clotet, Bonaventura; Borrell, Jose I.; Teixido, Jordi European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 159 - 174

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Citation Number: 12

Abstract

New analogues of 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) were synthesized and evaluated for their in vitro activities against HIV-1 in MT-4 cell cultures. Chemical diversity was introduced in 4 of the six positions of the core and the influence of each substituent was studied. This library was built on the basis of a rational diversity analysis with the objective of maximizing diversity and thus, the activity range with a ...