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Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Haddach, Mustapha; Michaux, Jerome; Schwaebe, Michael K; Pierre, Fabrice; O'Brien, Sean E; Borsan, Cosmin; Tran, Joe; Raffaele, Nicholas; Ravula, Suchitra; Drygin, Denis; Siddiqui-Jain, Adam; Darjania, Levan; Stansfield, Ryan; Proffitt, Chris; Macalino, Diwata; Streiner, Nicole; Bliesath, Joshua; Omori, May; Whitten, Jeffrey P; Anderes, Kenna; Rice, William G; Ryckman, David M.
Afiliación
  • Haddach M; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Michaux J; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Schwaebe MK; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Pierre F; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • O'Brien SE; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Borsan C; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Tran J; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Raffaele N; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Ravula S; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Drygin D; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Siddiqui-Jain A; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Darjania L; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Stansfield R; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Proffitt C; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Macalino D; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Streiner N; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Bliesath J; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Omori M; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Whitten JP; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Anderes K; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Rice WG; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
  • Ryckman DM; Cylene Pharmaceuticals Inc. , 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States.
ACS Med Chem Lett ; 3(2): 135-9, 2012 Feb 09.
Article en En | MEDLINE | ID: mdl-24900437
ABSTRACT
Structure-activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2012 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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PubMed Links
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2012 Tipo del documento: Article País de afiliación: Estados Unidos