Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives.
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.
Popowycz
Florence
F
Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, UMR-CNRS 5246, Université de Lyon, Université Claude Bernard-Lyon 1, Bâtiment Curien, Villeurbanne, France.
Schneider
Cédric
C
Debonis
Salvatore
S
Skoufias
Dimitrios A
DA
Kozielski
Frank
F
Galmarini
Carlos M
CM
Joseph
Benoît
B
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
D000970:Antineoplastic Agents; D011687:Purines; D011720:Pyrazoles; D014227:Triazines; D050257:Tubulin Modulators; C407365:myoseverin