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

A series of 4p-[(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 C4 beta-azido podophyllotoxin and C4 beta-azido-4'-O-demethy1 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.