Identification of 4, 5-dihydro-1 H-pyrazolo [4, 3-h] quinazoline derivatives as a new class of orally and selective polo-like kinase 1 inhibitors

I Beria, D Ballinari, JA Bertrand, D Borghi…

Index: Beria, Italo; Ballinari, Dario; Bertrand, Jay Aaron; Borghi, Daniela; Bossi, Roberto Tiberio; Brasca, Maria Gabriella; Cappella, Paolo; Caruso, Michele; Ceccarelli, Walter; Ciavolella, Antonella; Cristiani, Cinzia; Croci, Valter; De Ponti, Anna; Fachin, Gabriele; Ferguson, Ronald Dale; Lansen, Jacqueline; Moll, Jurgen Karl; Pesenti, Enrico; Posteri, Helena; Perego, Rita; Rocchetti, Maurizio; Storici, Paola; Volpi, Daniele; Valsasina, Barbara Journal of Medicinal Chemistry, 2010 , vol. 53, # 9 p. 3532 - 3551

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Citation Number: 52

Abstract

Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is recognized as an attractive therapeutic target in the treatment of proliferative diseases. Here we discuss the structure− activity relationship of the 4, 5-dihydro-1 H-pyrazolo [4, 3-h] quinazoline class of compounds that emerged from a high throughput screening (HTS) campaign as potent ...