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

A series of 4β-[(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 C4β-azido podophyllotoxin and C4β-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.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide