Ontology highlight
ABSTRACT:
SUBMITTER: Zhang W
PROVIDER: S-EPMC4148167 | biostudies-literature | 2014 Aug
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20140806 16
We previously reported a potent small molecule Mer tyrosine kinase inhibitor UNC1062. However, its poor PK properties prevented further assessment in vivo. We report here the sequential modification of UNC1062 to address DMPK properties and yield a new potent and highly orally bioavailable Mer inhibitor, 11, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kin ...[more]