1140904-19-3Relevant academic research and scientific papers
Synthesis and SAR of inhibitors of protein kinase CK2: Novel tricyclic quinoline analogs
Haddach, Mustapha,Pierre, Fabrice,Regan, Collin F.,Borsan, Cosmin,Michaux, Jerome,Stefan, Eric,Kerdoncuff, Pauline,Schwaebe, Michael K.,Chua, Peter C.,Siddiqui-Jain, Adam,MacAlino, Diwata,Drygin, Denis,O'Brien, Sean E.,Rice, William G.,Ryckman, David M.
scheme or table, p. 45 - 48 (2012/02/04)
Protein kinase CK2 is a potential drug target for many diseases including cancer and inflammation disorders. The crystal structure of clinical candidate CX-4945 1 with CK2 revealed an indirect interaction with the protein through hydrogen bonding between the NH of the 3-chlorophenyl amine and a water molecule. Herein, we investigate the relevance of this hydrogen bond by preparing several novel tricyclic derivatives lacking a NH moiety at the same position. This SAR study allowed the discovery of highly potent CK2 inhibitors.
THERAPEUTIC KINASE MODULATORS
-
Page/Page column 43, (2009/04/24)
The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, and modulating protein kinase activity. Molecules of the invention can modulate casein kinase (CK) activity. The invention also relates in part to methods for using such molecules.
