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

Italo Beria,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

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

A 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline series of Polo-like kinase inhibitors is reported and the SAR disclosed. The series led to low nanomolar PLK1 inhibitors. Compound 4 was tested in vivo showing good antitumor efficacy after iv administration.

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关键词

PLK1,Polo-like kinase,Kinase inhibitor,In vivo activity

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