Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.
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.
Scott
David A
DA
Cancer Research, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
Aquila
Brian M
BM
Bebernitz
Geraldine A
GA
Cook
Donald J
DJ
Dakin
Les A
LA
Deegan
Tracy L
TL
Hattersley
Maureen M
MM
Ioannidis
Stephanos
S
Lyne
Paul D
PD
Omer
Charles A
CA
Ye
Minwei
M
Zheng
Xiaolan
X
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*
D000577:Amides; D000970:Antineoplastic Agents; D013844:Thiazoles; D016186:Receptor, Macrophage Colony-Stimulating Factor