title: Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors.
abstract: Our continued effort toward the development of the imidazo[1,2-a]pyrazine scaffold as Aurora kinase inhibitors is described. Bioisosteric approach was applied to optimize the 8-position of the core. Several new potent Aurora A/B dual inhibitors, such as 25k and 25l, were identified.
authors.affiliation: Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States. zhaoyang.meng@merck.com
authors.forename: Zhaoyang
authors.initials: Z
authors.lastname: Meng
authors.forename: Bheemashankar A
authors.initials: BA
authors.lastname: Kulkarni
authors.forename: Angela D
authors.initials: AD
authors.lastname: Kerekes
authors.forename: Amit K
authors.initials: AK
authors.lastname: Mandal
authors.forename: Sara J
authors.initials: SJ
authors.lastname: Esposite
authors.forename: David B
authors.initials: DB
authors.lastname: Belanger
authors.forename: Panduranga Adulla
authors.initials: PA
authors.lastname: Reddy
authors.forename: Andrea D
authors.initials: AD
authors.lastname: Basso
authors.forename: Seema
authors.initials: S
authors.lastname: Tevar
authors.forename: Kimberly
authors.initials: K
authors.lastname: Gray
authors.forename: Jennifer
authors.initials: J
authors.lastname: Jones
authors.forename: Elizabeth B
authors.initials: EB
authors.lastname: Smith
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Doll
authors.forename: M Arshad
authors.initials: MA
authors.lastname: Siddiqui
mesh_terms: D000818:Animals; D064096:Aurora Kinase A; D064127:Aurora Kinases; D004353:Drug Evaluation, Preclinical; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats
chemical_list: D007093:Imidazoles; D047428:Protein Kinase Inhibitors; D011719:Pyrazines; C576920:Aurka protein, rat; D064096:Aurora Kinase A; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases