title: Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
abstract: The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile.
authors.affiliation: Department of Chemistry, Merck Research Laboratories, Cambridge, MA 02141, USA. david.belanger@merck.com
authors.forename: David B
authors.initials: DB
authors.lastname: Belanger
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Curran
authors.forename: Alan
authors.initials: A
authors.lastname: Hruza
authors.forename: Johannes
authors.initials: J
authors.lastname: Voigt
authors.forename: Zhaoyang
authors.initials: Z
authors.lastname: Meng
authors.forename: Amit K
authors.initials: AK
authors.lastname: Mandal
authors.forename: M Arshad
authors.initials: MA
authors.lastname: Siddiqui
authors.forename: Andrea D
authors.initials: AD
authors.lastname: Basso
authors.forename: Kimberly
authors.initials: K
authors.lastname: Gray
mesh_terms: D064127:Aurora Kinases; D001798:Blood Proteins / Q000378:metabolism; D018360:Crystallography, X-Ray; D055808:Drug Discovery; D005434:Flow Cytometry; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011719:Pyrazines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D001798:Blood Proteins; D007093:Imidazoles; D047428:Protein Kinase Inhibitors; D011719:Pyrazines; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases