Ontology highlight
ABSTRACT:
SUBMITTER: Huang A
PROVIDER: S-EPMC4716597 | biostudies-literature | 2016 Jan
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20151202 1
Efforts to identify a potent, reversible, nonsteroidal CYP17A1 lyase inhibitor with good selectivity over CYP17A1 hydroxylase and CYPs 11B1 and 21A2 for the treatment of castration-resistant prostate cancer (CRPC) culminated in the discovery of BMS-351 (compound 18), a pyridyl biaryl benzimidazole with an excellent in vivo profile. Biological evaluation of BMS-351 at a dose of 1.5 mg in castrated cynomolgus monkeys revealed a remarkable reduction in testosterone levels with minimal glucocorticoi ...[more]