title: Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.
abstract: The bisamide class of kinase inhibitors was identified as being active against CSF-1R. The synthesis and SAR of pyridyl and thiazolyl bisamides are reported, along with the pharmacokinetic properties and in vivo activity of selected examples.
authors.affiliation: Cancer Research, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
authors.forename: David A
authors.initials: DA
authors.lastname: Scott
authors.forename: Brian M
authors.initials: BM
authors.lastname: Aquila
authors.forename: Geraldine A
authors.initials: GA
authors.lastname: Bebernitz
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Cook
authors.forename: Les A
authors.initials: LA
authors.lastname: Dakin
authors.forename: Tracy L
authors.initials: TL
authors.lastname: Deegan
authors.forename: Maureen M
authors.initials: MM
authors.lastname: Hattersley
authors.forename: Stephanos
authors.initials: S
authors.lastname: Ioannidis
authors.forename: Paul D
authors.initials: PD
authors.lastname: Lyne
authors.forename: Charles A
authors.initials: CA
authors.lastname: Omer
authors.forename: Minwei
authors.initials: M
authors.lastname: Ye
authors.forename: Xiaolan
authors.initials: X
authors.lastname: Zheng
mesh_terms: D016475:3T3 Cells; D000577:Amides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D005260:Female; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism*; D051381:Rats; D016186:Receptor, Macrophage Colony-Stimulating Factor / Q000037:antagonists & inhibitors* / Q000235:genetics; D013844:Thiazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D013844:Thiazoles; D016186:Receptor, Macrophage Colony-Stimulating Factor