Pyrazolo [3, 4-c] pyridazines as novel and selective inhibitors of cyclin-dependent kinases

…, F Llinares, D Munoz-Mingarro, O Lozach…

Index: Brana, Miguel F.; Cacho, Monica; Garcia, M. Luisa; Mayoral, Elena P.; Lopez, Berta; De Pascual-Teresa, Beatriz; Ramos, Ana; Acero, Nuria; Llinares, Francisco; Munoz-Mingarro, Dolores; Lozach, Olivier; Meijer, Laurent Journal of Medicinal Chemistry, 2005 , vol. 48, # 22 p. 6843 - 6854

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Citation Number: 67

Abstract

Pyrazolopyridazine 1a was identified in a high-throughput screening carried out by BASF Bioresearch Corp.(Worcester, MA) as a potent inhibitor of CDK1/cyclin B and shown to have selectivity for the CDK family. Analogues of the lead compound have been synthesized and their antitumor activities have been tested. A molecular model of the complex between the lead compound and the CDK2 ATP binding site has been built using a combination of ...