912366-83-7Relevant academic research and scientific papers
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors
Zhao, Lianyun,Zhang, Yingxin,Dai, Chaoyang,Guzi, Timothy,Wiswell, Derek,Seghezzi, Wolfgang,Parry, David,Fischmann, Thierry,Siddiqui, M. Arshad
scheme or table, p. 7216 - 7221 (2011/01/03)
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 1 nM.
SUBSTITUTED HETEROCYCLES AND THEIR USE AS CHK1, PDK1 AND PAK INHIBITORS
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Page/Page column 59, (2008/06/13)
This invention relates to novel compounds of Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess CHK1 kinase inhibitory activity, PDK1 inhibitory activity and Pak kinase inhibitory activity and are accordingly useful in the treatment and/or prophylaxis of cancer.
