Synthesis and cytotoxic evaluation of novel amide-triazole-linked triterpenoid-AZT conjugates

A variety of triterpenoid propargyl amides, prepared from the corresponding acids, was used as substrates for the construction of novel triazole-tethered triterpenoid-AZT conjugates via a click chemistry-mediated coupling with azidothymidine (AZT). Thus, nineteen new hybrids were successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity of four triterpenoid AZT hybrids on KB and Hep-G2 tumor cell lines. (C) 2014 Elsevier Ltd. All rights reserved.