1034616-40-4Relevant 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
, p. 6489 - 6494 (2010)
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.
