1.
Bioorg Med Chem Lett
; 16(21): 5561-6, 2006 Nov 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16934458
RESUMEN
The development of potent, orally bioavailable, and selective series of 5-amino-3-hydroxy-N(1-hydroxypropane-2-yl)isothiazole-4-carboxamidine inhibitors of MEK1 and MEK-2 kinase is described. Optimization of the carboxamidine and the phenoxyaniline group led to the identification of 55 which gave good potency as in vitro MEK1 inhibitors, and good oral exposure in rat.
Asunto(s)
Amidinas/farmacología , MAP Quinasa Quinasa 1/antagonistas & inhibidores , Regulación Alostérica , Amidinas/síntesis química , Amidinas/química , Animales , MAP Quinasa Quinasa 2/antagonistas & inhibidores , Ratas
2.
Bioorg Med Chem Lett
; 16(15): 3975-80, 2006 Aug 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16725322
RESUMEN
3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles were discovered as potent in vitro MEK1 inhibitors.