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. 2010 Nov 15;20(22):6489-94.
doi: 10.1016/j.bmcl.2010.09.060. Epub 2010 Sep 17.

4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors

Italo Beria  1 , Barbara Valsasina, Maria Gabriella Brasca, Walter Ceccarelli, Maristella Colombo, Sabrina Cribioli, Gabriele Fachin, Ronald D Ferguson, Francesco Fiorentini, Laura M Gianellini, Maria L Giorgini, Jurgen K Moll, Helena Posteri, Daniele Pezzetta, Fulvia Roletto, Francesco Sola, Dania Tesei, Michele Caruso
Affiliations

4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors

Italo Beria et al. Bioorg Med Chem Lett. .

Abstract

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 i.v. administration.

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