1.
Bioorg Med Chem Lett
; 18(23): 6171-4, 2008 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18951019
RESUMO
This paper reports a second generation MEK inhibitor. The previously reported potent and efficacious MEK inhibitor, PD-184352 (CI-1040), contains an integral hydroxamate moiety. This compound suffered from less than ideal solubility and metabolic stability. An oxadiazole moiety behaves as a bioisostere for the hydroxamate group, leading to a more metabolically stable and efficacious MEK inhibitor.