Synthesis and identification of [1, 3, 5] triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors

…, A Fuentes-Pesquera, SA Middleton…

Index: Kuo, Gee-Hong; DeAngelis, Alan; Emanuel, Stuart; Wang, Aihua; Zhang, Yan; Connolly, Peter J.; Chen, Xin; Gruninger, Robert H.; Rugg, Catherine; Fuentes-Pesquera, Angel; Middleton, Steven A.; Jolliffe, Linda; Murray, William V. Journal of Medicinal Chemistry, 2005 , vol. 48, # 14 p. 4535 - 4546

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Citation Number: 79

Abstract

On the basis of previous studies, we identified pyrazine-pyridine A as a potent vascular endothelial growth factor inhibitor and pyrimidine-pyridine B as a moderately potent cyclin dependent kinase (CDK) inhibitor. A proposed combination of CGP-60474 and compound B led to the discovery of [1, 3, 5] triazine-pyridine as a new series of potent CDK inhibitors. Palladium-catalyzed CC bond formation reactions, particularly the Negishi coupling ...