Ontology highlight
ABSTRACT:
SUBMITTER: Liu G
PROVIDER: S-EPMC4025831 | biostudies-other | 2012 Dec
REPOSITORIES: biostudies-other
Liu Gang G Campbell Brian T BT Holladay Mark W MW Ford Pulido Julia M JM Hua Helen H Gitnick Dana D Gardner Michael F MF James Joyce J Breider Mike A MA Brigham Daniel D Belli Barbara B Armstrong Robert C RC Treiber Daniel K DK
ACS medicinal chemistry letters 20120924 12
A series of potent, selective platelet-derived growth factor receptor-family kinase inhibitors was optimized starting from a globally selective lead molecule 4 through structural modifications aimed at improving the physiochemical and pharmacokinetic properties, as exemplified by 18b. Further clearance reduction via per-methylation of the α-carbons of a solubilizing piperidine nitrogen resulted in advanced leads 22a and 22b. Results from a mouse tumor xenograft, a collagen-induced arthritis mode ...[more]