Your browser doesn't support javascript.
loading
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Bandarage, Upul K; Cao, Jingrong; Come, Jon H; Court, John J; Gao, Huai; Jacobs, Marc D; Marhefka, Craig; Nanthakumar, Suganthi; Green, Jeremy.
Afiliación
  • Bandarage UK; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA. Electronic address: upul_bandarage@vrtx.com.
  • Cao J; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Come JH; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Court JJ; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Gao H; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Jacobs MD; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Marhefka C; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Nanthakumar S; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
  • Green J; Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA. Electronic address: jeremy_green@vrtx.com.
Bioorg Med Chem Lett ; 28(15): 2622-2626, 2018 08 15.
Article en En | MEDLINE | ID: mdl-30082069
ABSTRACT
Rho kinase (ROCK) inhibitors are potential therapeutic agents for the treatment of a variety of disorders including hypertension, glaucoma and erectile dysfunction. Here we disclose a series of potent and selective ROCK inhibitors based on a substituted 7-azaindole scaffold. Substitution of the 3-position of 7-azaindole led to compounds such as 37, which possess excellent ROCK inhibitory potency and high selectivity against the closely related kinase PKA.
Asunto(s)
Palabras clave
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Inhibidores de Proteínas Quinasas / Quinasas Asociadas a rho / Indoles Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Inhibidores de Proteínas Quinasas / Quinasas Asociadas a rho / Indoles Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article