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 podophyl...

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Published inArchiv der Pharmazie (Weinheim) Vol. 341; no. 2; pp. 126 - 131
Main Authors Reddy, Pitta B, Paul, David V, Agrawal, Satyam K, Saxena, Ajit K, Kumar, Halmuthur M S, Qazi, Ghulam N
Format Journal Article
LanguageEnglish
Published Germany 01.02.2008
Subjects
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Line, Tumor
Drug Screening Assays, Antitumor
Humans
Podophyllotoxin - analogs & derivatives
Podophyllotoxin - chemical synthesis
Podophyllotoxin - chemistry
Podophyllotoxin - pharmacology
Structure-Activity Relationship
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
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Summary: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.
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ISSN:0365-6233
DOI:10.1002/ardp.200700116