1034616-38-0Relevant academic research and scientific papers
4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors
Beria, Italo,Valsasina, Barbara,Brasca, Maria Gabriella,Ceccarelli, Walter,Colombo, Maristella,Cribioli, Sabrina,Fachin, Gabriele,Ferguson, Ronald D.,Fiorentini, Francesco,Gianellini, Laura M.,Giorgini, Maria L.,Moll, Jurgen K.,Posteri, Helena,Pezzetta, Daniele,Roletto, Fulvia,Sola, Francesco,Tesei, Dania,Caruso, Michele
supporting information; experimental part, p. 6489 - 6494 (2011/01/12)
A series of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives was optimized as Polo-like kinase 1 inhibitors. Extensive SAR afforded a highly potent and selective PLK1 compound. The compound showed good antiproliferative activity when tested in a panel of tumor cell lines with PLK1 related mechanism of action and with good in vivo antitumor efficacy in two xenograft models after iv administration.
SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 74; 75, (2008/12/06)
Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may
