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

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.

journal_name

Bioorg Med Chem Lett

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

doi

10.1016/j.bmcl.2014.09.079

subject

Has Abstract

pub_date

2014-11-15 00:00:00

pages

5190-4

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01035-X

journal_volume

24

pub_type

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