Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents

Yu Hsiang Lo, Ying Ting Lin, Yu Peng Liu, Tsai Hui Duh, Pei Jung Lu, Ming Jung Wu

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

A series of novel enediyne-containing molecules, 1-aryl-6-(3,4,5- trimethoxyphenyl)-3(Z)-hexen-1,5-diynes, were synthesized and displayed significant IC50 values of 10-7 to 10-6 M against various cancer cell lines. Of these compounds, 1-(2-pyridinyl)-6-(3,4,5- trimethoxyphenyl)-3(Z)-hexen-1,5-diyne (8) demonstrated the greatest growth inhibition activity. Compound 8 also arrested cancer cells in the G2/M phase and induced apoptosis via activation of Caspase-3. In addition to the G2/M block, compound 8 caused microtubule depolymerization at low concentrations and markedly decreased tumor size in xenographic studies.

Original languageEnglish
Pages (from-to)526-533
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume62
DOIs
Publication statusPublished - 2013 Apr

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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