Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors

…, D Wiswell, W Seghezzi, D Parry, T Fischmann…

文献索引：Zhao, Lianyun; Zhang, Yingxin; Dai, Chaoyang; Guzi, Timothy; Wiswell, Derek; Seghezzi, Wolfgang; Parry, David; Fischmann, Thierry; Siddiqui, M. Arshad Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7216 - 7221

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被引用次数: 25

摘要

A novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1nM.