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Eur J Med Chem. 2008 Oct;43(10):2067-72. Epub 2007 Sep 29.

Studies on novel 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxins as potential anticancer agents.

Author information

1
Synthetic Chemistry Division, Pharmacology Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu-Tawi 180001, India.

Abstract

A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxin congeners have been designed and synthesized with significant regioselectivity by employing Cu(I) catalyzed 1,3-dipolar cycloaddition reaction of C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin with N-prop-2-yn-1-ylanilines. These compounds were evaluated for anticancer activity against a panel of seven human cancer cell lines. It was interesting to note that all the compounds exhibited promising activity especially against SF-295 (CNS), HCT-15 (colon) and 502713 (colon) cell lines. Compound 11e was found to be the most promising in this study.

PMID:
17988764
DOI:
10.1016/j.ejmech.2007.09.015
[Indexed for MEDLINE]

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