Design, synthesis, and biological testing of 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin analogues as antitumor agents.

A series of 4beta-[(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 C4beta-azido podophyllotoxin and C4beta-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.