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Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs
Authors: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
Institution:Cylene Pharmaceuticals Inc., 5820 Nancy Ridge Drive, Suite 200, San Diego, CA 92121, USA. mhaddach@cylenepharma.com
Abstract: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.
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