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  • Title: 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.
    Author: Beria I, Valsasina B, Brasca MG, Ceccarelli W, Colombo M, Cribioli S, Fachin G, Ferguson RD, Fiorentini F, Gianellini LM, Giorgini ML, Moll JK, Posteri H, Pezzetta D, Roletto F, Sola F, Tesei D, Caruso M.
    Journal: Bioorg Med Chem Lett; 2010 Nov 15; 20(22):6489-94. PubMed ID: 20932759.
    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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