title: Studies on novel 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxins as potential anticancer agents.
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.
authors.affiliation: Synthetic Chemistry Division, Pharmacology Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu-Tawi 180001, India.
authors.forename: Bilal A
authors.initials: BA
authors.lastname: Bhat
authors.forename: P Bhaskar
authors.initials: PB
authors.lastname: Reddy
authors.forename: Satyam Kumar
authors.initials: SK
authors.lastname: Agrawal
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
authors.forename: H M Sampath
authors.initials: HM
authors.lastname: Kumar
authors.forename: G N
authors.initials: GN
authors.lastname: Qazi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D011034:Podophyllotoxin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D013379:Substrate Specificity; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D014230:Triazoles; D011034:Podophyllotoxin