title: Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.
abstract: In an effort to discover Aurora kinase inhibitors, an HTS hit revealed an amide containing pyrrolopyrimidine compound. Replacement of the pyrrolopyrimidine residue with a thienopyrimidine moiety led to a series of potent and selective Aurora inhibitors.
authors.affiliation: Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. william.j.mcclellan@abbott.com
authors.forename: William J
authors.initials: WJ
authors.lastname: McClellan
authors.forename: Yujia
authors.initials: Y
authors.lastname: Dai
authors.forename: Cele
authors.initials: C
authors.lastname: Abad-Zapatero
authors.forename: Daniel H
authors.initials: DH
authors.lastname: Albert
authors.forename: Jennifer J
authors.initials: JJ
authors.lastname: Bouska
authors.forename: Keith B
authors.initials: KB
authors.lastname: Glaser
authors.forename: Terry J
authors.initials: TJ
authors.lastname: Magoc
authors.forename: Patrick A
authors.initials: PA
authors.lastname: Marcotte
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Osterling
authors.forename: Kent D
authors.initials: KD
authors.lastname: Stewart
authors.forename: Steven K
authors.initials: SK
authors.lastname: Davidsen
authors.forename: Michael R
authors.initials: MR
authors.lastname: Michaelides
mesh_terms: D000818:Animals; D064127:Aurora Kinases; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D057166:High-Throughput Screening Assays; D006860:Hydrogen Bonding; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; C476003:thienopyrimidine; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases