Synthesis and cytotoxic evaluation of betulin-triazole-AZT hybrids

Abstract

Betulin was converted to the corresponding alkyne-functionalized esters and amides and subsequently deployed as substrates for a 'click' chemistry-mediated coupling with 3'-azido-3'-deoxythydimine (AZT) to furnish a novel betulin-triazole-AZT hybrid compounds. Eleven new hybrids were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.