Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives

  • Bioorg Med Chem. 2009 May 1;17(9):3471-8. doi: 10.1016/j.bmc.2009.03.007.
Florence Popowycz  1 ,  Cédric Schneider ,  Salvatore Debonis ,  Dimitrios A Skoufias ,  Frank Kozielski ,  Carlos M Galmarini ,  Benoît Joseph
Affiliations
  • 1. Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, UMR-CNRS 5246, Université de Lyon, Université Claude Bernard-Lyon 1, Bâtiment Curien, Villeurbanne, France.
PMID: 19349183 DOI: 10.1016/j.bmc.2009.03.007
Abstract

Pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives 1a-c were prepared from 4-(N-methyl-N-phenylamino)-2-methylsulfanylpyrazolo[1,5-a]-1,3,5-triazine 2. Their cytotoxic activity, inhibition of tubulin polymerization, and cell cycle effects were evaluated. Compounds 1a and 1c are potent tubulin inhibitors and displayed specific antiproliferative activity in colorectal Cancer cell lines at micromolar concentrations.