Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase

…, Y Yan, S Munshi, M Ikuta, L Kuo, C Kreatsoulas…

Index: Garbaccio, Robert M.; Huang, Shaei; Tasber, Edward S.; Fraley, Mark E.; Yan, Youwei; Munshi, Sanjeev; Ikuta, Mari; Kuo, Lawrence; Kreatsoulas, Constanine; Stirdivant, Steve; Drakas, Bob; Rickert, Keith; Walsh, Eileen S.; Hamilton, Kelly A.; Buser, Carolyn A.; Hardwick, James; Mao, Xianzhi; Beck, Stephen C.; Abrams, Marc T.; Tao, Weikang; Lobell, Rob; Sepp-Lorenzino, Laura; Hartman, George D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 22 p. 6280 - 6285

Full Text: HTML

Citation Number: 19

Abstract

From HTS lead 1, a novel benzoisoquinolinone class of ATP-competitive Chk1 inhibitors was devised and synthesized via a photochemical route. Using X-ray crystallography as a guide, potency was rapidly enhanced through the installation of a tethered basic amine ...