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

Basic Information

ID: ALA3351916

Journal: Bioorg Med Chem Lett

Title: Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates.

Authors: Dang Thi TA, Kim Tuyet NT, Pham The C, Thanh Nguyen H, Ba Thi C, Doan Duy T, D'hooghe M, Van Nguyen T.

Abstract: Betulinic acid and analogous naturally occurring triterpenoid acids were transformed into the corresponding propargyl esters and subsequently deployed as substrates for a click chemistry-mediated coupling with azidothymidine (AZT) en route to novel 1,2,3-triazole-tethered triterpenoid-AZT conjugates. Twelve new hybrids were thus prepared and assessed in terms of their cytotoxic activity, revealing an interesting anticancer activity of five triterpenoid-AZT hybrids on KB and Hep-G2 tumor cell lines.

CiteXplore: 25442310

DOI: 10.1016/j.bmcl.2014.09.079

Patent ID: