Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2009

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

Résumé

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.

Domaines

Chimie organique

Dates et versions

hal-00691448 , version 1 (26-04-2012)

Identifiants

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Florence Popowycz, Cédric Schneider, Salvatore Debonis, Dimitrios Skoufias, Frank Kozielski, et al.. Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives.. Bioorganic and Medicinal Chemistry, 2009, 17 (9), pp.3471-8. ⟨10.1016/j.bmc.2009.03.007⟩. ⟨hal-00691448⟩
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