Synthesis and biological evaluation of 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxins as potential anticancer agents

Chem Biodivers. 2008 Sep;5(9):1792-802. doi: 10.1002/cbdv.200890168.

Abstract

A series of novel 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin derivatives were synthesized by employing Cu(I)-catalyzed click chemistry and evaluated for their anticancer activity against a panel of seven human cancer cell lines (HT-29, HCT-15, 502713, HOP-62, A-549, MCF-7, and SF-295). The compounds 9b, 9c, 9e, 9f, and 9h showed significant cytotoxic activities especially against HT-29, HCT-15, 502713 cell lines.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Podophyllotoxin / chemical synthesis*
  • Podophyllotoxin / chemistry
  • Podophyllotoxin / pharmacology*
  • Structure-Activity Relationship
  • Triazoles / chemistry*

Substances

  • Antineoplastic Agents
  • Triazoles
  • Podophyllotoxin