NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Italo Beria,Roberto T Bossi,Maria Gabriella Brasca,Michele Caruso,Walter Ceccarelli,Gabriele Fachin,Marina Fasolini,Barbara Forte,Francesco Fiorentini,Enrico Pesenti,Daniele Pezzetta,Helena Posteri,Alessandra Scolaro,Stefania Re Depaolini,Barbara Valsasina

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

Lead optimization work on the 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline series led to identification of NMS-P937. Crystal structure of NMS-P937 with PLK1 was obtained and discussed. NMS-P937 is a potent, selective and orally available PLK1 inhibitor that is presently in Phase I clinical trials.

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关键词

PLK1,Polo-like kinase,Kinase inhibitor,In vivo activity,Phase I clinical trials

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