Your browser doesn't support javascript.
loading
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.
Harikrishnan, Lalgudi S; Gill, Patrice; Kamau, Muthoni G; Qin, Lan-Ying; Ruan, Zheming; O'Malley, Daniel; Huynh, Tram; Stachura, Sylwia; Cavallaro, Cullen L; Lu, Zhonghui; J-W Duan, James; Weigelt, Carolyn A; Sack, John S; Ruzanov, Max; Khan, Javed; Gururajan, Murali; Wong, Jessica J; Huang, Yanling; Yarde, Melissa; Li, Zhuyin; Chen, Cliff; Sun, Huadong; Borowski, Virna; Murtaza, Anwar; Fink, Brian E.
Afiliação
  • Harikrishnan LS; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA. Electronic address: lalgudi.harikrishnan@bms.com.
  • Gill P; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Kamau MG; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Qin LY; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Ruan Z; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • O'Malley D; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Huynh T; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Stachura S; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Cavallaro CL; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Lu Z; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • J-W Duan J; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Weigelt CA; Molecular Structure & Design, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Sack JS; Molecular Structure & Design, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Ruzanov M; Molecular Structure & Design, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Khan J; Molecular Structure & Design, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Gururajan M; Immuno-Oncology Small Molecule Biology, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Wong JJ; Immuno-Oncology Small Molecule Biology, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Huang Y; Immuno-Oncology Small Molecule Biology, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Yarde M; Lead Discovery & Optimization, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Li Z; Lead Discovery & Optimization, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Chen C; Preclinical Candidate Optimization, MAP, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Sun H; Preclinical Candidate Optimization, MAP, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Borowski V; In vivo Pharmacology, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Murtaza A; In vivo Pharmacology, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
  • Fink BE; Department of Chemistry, Bristol Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA.
Bioorg Med Chem Lett ; 30(12): 127204, 2020 06 15.
Article em En | MEDLINE | ID: mdl-32334911
Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in an MC38 mouse tumor model, demonstrated a desired pharmacokinetic profile as well as a dose-dependent pharmacodynamic response. However, no perceptible efficacy was observed in this tumor model at the doses investigated.
Assuntos
Palavras-chave
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Benzil / Receptores do Ácido Retinoico / Compostos Heterocíclicos Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2020 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Benzil / Receptores do Ácido Retinoico / Compostos Heterocíclicos Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2020 Tipo de documento: Article