1140904-15-9Relevant 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.
