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Design, Synthesis, and Biological Testing of 4β‐[(4‐Substituted)‐1,2,3‐triazol‐1‐yl]podophyllotoxin Analogues as Antitumor Agents
Author(s) -
Reddy Pitta B.,
Paul David V.,
Agrawal Satyam K.,
Saxena Ajit K.,
Kumar Halmuthur M. S.,
Qazi Ghulam N.
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700116
Subject(s) - podophyllotoxin , chemistry , cycloaddition , stereochemistry , selectivity , propargyl , biological activity , cell culture , triazole , combinatorial chemistry , biochemistry , in vitro , organic chemistry , catalysis , biology , genetics
A series of 4β‐[(4‐substituted)‐1,2,3‐triazol‐1‐yl]podophyllotoxin analogues have been synthesized with high regio‐selectivity by employing copper(I)‐catalyzed 1,3‐dipolar cycloaddition of 1‐ O ‐propargyl monosaccharides with C4β‐azido podophyllotoxin and C4β‐azido‐4′‐ O ‐demethyl podophyllotoxin. All the compounds were evaluated for their anticancer activity against a panel of six human cancer cell lines. Among these, 4′‐ O ‐demethyl podophyllotoxin congeners are showing promising anticancer activity mainly against HCT‐15 (colon) and DU‐145 (prostate) cells.