Your browser doesn't support javascript.
loading
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.
Markwalder, Jay A; Seitz, Steven P; Blat, Yuval; Elkin, Lisa; Hunt, John T; Pabalan, Jonathan G; Jure-Kunkel, Maria N; Vite, Gregory D; Covello, Kelly.
Afiliação
  • Markwalder JA; Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States. Electronic address: jay.markwalder@bms.com.
  • Seitz SP; Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
  • Blat Y; Mechanistic Biochemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
  • Elkin L; Lead Discovery & Optimization, Bristol-Myers Squibb Research and Development, Wallingford, CT 06492, United States.
  • Hunt JT; Oncology Biology, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
  • Pabalan JG; Oncology Biology, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
  • Jure-Kunkel MN; Oncology Biology, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
  • Vite GD; Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
  • Covello K; Oncology Biology, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
Bioorg Med Chem Lett ; 27(3): 582-585, 2017 02 01.
Article em En | MEDLINE | ID: mdl-28003141
ABSTRACT
The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.
Assuntos
Palavras-chave
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ureia / Ácidos Carboxílicos / Inibidores Enzimáticos / Indolamina-Pirrol 2,3,-Dioxigenase Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ureia / Ácidos Carboxílicos / Inibidores Enzimáticos / Indolamina-Pirrol 2,3,-Dioxigenase Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article