Your browser doesn't support javascript.
loading
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.
Brown, Gregory D; Shi, Qing; Delucca, George V; Batt, Douglas G; Galella, Michael A; Cvijic, Mary-Ellen; Liu, Rui-Qin; Qiu, Feng; Zhao, Qihong; Barrish, Joel C; Carter, Percy H.
Afiliação
  • Brown GD; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States. Electronic address: gregory.brown@bms.com.
  • Shi Q; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Delucca GV; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Batt DG; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Galella MA; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Cvijic ME; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Liu RQ; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Qiu F; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Zhao Q; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Barrish JC; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
  • Carter PH; Research and Development, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ 08543-4000, United States.
Bioorg Med Chem Lett ; 26(2): 662-666, 2016 Jan 15.
Article em En | MEDLINE | ID: mdl-26631321
A novel cyclohexenyl series of CCR2 antagonists has been discovered. This series of small, rigid compounds exhibits submicromolar binding affinity for CCR2. Modification of the substituents on the cyclohexene ring led to the identification of potent CCR2 antagonists. Progress from initial lead 5 (IC50=700nM) to (-)-38 (IC50=9.0nM) is discussed.
Assuntos
Palavras-chave
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Cicloexenos / Receptores CCR2 Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Cicloexenos / Receptores CCR2 Idioma: En Ano de publicação: 2016 Tipo de documento: Article