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.
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Institut de Chimie et Biochimie Moleculaires et Supramoleculaires, UMR-CNRS 5246, Universite de Lyon, Universite Claude Bernard-Lyon 1, Batiment Curien, Villeurbanne, France.;
