title: Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase.
abstract: 3-amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.
authors.affiliation: Cancer Research, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. david.scott@astrazeneca.com
authors.forename: David A
authors.initials: DA
authors.lastname: Scott
authors.forename: Carrie L
authors.initials: CL
authors.lastname: Balliet
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Cook
authors.forename: Audrey M
authors.initials: AM
authors.lastname: Davies
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Gero
authors.forename: Charles A
authors.initials: CA
authors.lastname: Omer
authors.forename: Srinivasu
authors.initials: S
authors.lastname: Poondru
authors.forename: Maria-Elena
authors.initials: ME
authors.lastname: Theoclitou
authors.forename: Boris
authors.initials: B
authors.lastname: Tyurin
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Zinda
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D009369:Neoplasms / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D011804:Quinolines / Q000737:chemistry* / Q000493:pharmacokinetics*; D051381:Rats; D016186:Receptor, Macrophage Colony-Stimulating Factor / Q000037:antagonists & inhibitors* / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011804:Quinolines; D016186:Receptor, Macrophage Colony-Stimulating Factor