Twenty analogues of the anti-HIV-1 integrase (IN) inhibitors dicaffeoylquinic acids (DCQAs) were prepared. Their IC50 values
for 3’-end processing and strand transfer against recombinant HIV-1IN were determined in vitro, and their cell toxicities and EC50 against
HIV-1 were measured in cells (ex vivo). Acetylated or benzylated and/or with cyclohexylidene group compounds exhibited no inhibition
of integration in biochemical assays or viral replication in HIV-infected cells, with the exception of 16 and 36. Removal of these groups,
however, correlated with potent inhibition. Compounds 19, 31, and 38, all digalloyls, exhibited the most robust inhibitory performance in
biochemical assays as well as in cell culture and less toxicity than other molecules in the current study.
Keywords: Integrase inhibitor, HIV-1, dicaffeoyl, digalloyl, second generation inhibitor, esters, quinic acid, cyclitol, anti-HIV agents, catechol.
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Published on: 28 January, 2013
Page: [724 - 733]