Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives
作者:Florence Popowycz、Cédric Schneider、Salvatore DeBonis、Dimitrios A. Skoufias、Frank Kozielski、Carlos M. Galmarini、Benoît Joseph
DOI:10.1016/j.bmc.2009.03.007
日期:2009.5
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