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Design, Synthesis, and Biological Testing of 4β-[(4-Substituted)-1,2,3-triazol-1-yl]podophyllotoxin Analogues as Antitumor Agents

✍ Scribed by Pitta B. Reddy; David V. Paul; Satyam K. Agrawal; Ajit K. Saxena; Halmuthur M. S. Kumar; Ghulam N. Qazi

Publisher: John Wiley and Sons
Year: 2008
Tongue: English
Weight: 495 KB
Volume: 341
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.200700116

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✦ Synopsis

Abstract

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.

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