Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases

…, P Retailleau, BI Iorga, L Meijer, F Guéritte

Index: Nguyen, Thanh Binh; Lozach, Olivier; Surpateanu, Georgiana; Wang, Qian; Retailleau, Pascal; Iorga, Bogdan I.; Meijer, Laurent; Gueritte, Francoise Journal of Medicinal Chemistry, 2012 , vol. 55, # 6 p. 2811 - 2819

Full Text: HTML

Citation Number: 18

Abstract

The screening of the ICSN chemical library on various disease-relevant protein kinases led to the identification of natural flavonoidal alkaloids of unknown configuration as potent inhibitors of the CDK1 and CDK5 kinases. We thus developed an efficient and modular synthetic strategy for their preparation and that of analogues in order to determine the absolute configuration of the active natural flavonoidal alkaloids and to provide further ...