| First Author | Huang A | Year | 2016 |
| Journal | ACS Med Chem Lett | Volume | 7 |
| Issue | 1 | Pages | 40-5 |
| PubMed ID | 26819663 | Mgi Jnum | J:354408 |
| Mgi Id | MGI:7734802 | Doi | 10.1021/acsmedchemlett.5b00310 |
| Citation | Huang A, et al. (2016) Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer. ACS Med Chem Lett 7(1):40-5 |
| abstractText | 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 glucocorticoid and mineralcorticoid perturbation. Based on a favorable profile, BMS-351 was selected as a candidate for further preclinical evaluation. |
