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Bioorg Med Chem Lett
; 20(22): 6489-94, 2010 Nov 15.
Article
in English
| MEDLINE
| ID: mdl-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.