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Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.
Caldwell, Timothy M; Kaufman, Michael D; Wise, Scott C; Mi Ahn, Yu; Hood, Molly M; Lu, Wei-Ping; Patt, William C; Samarakoon, Thiwanka; Vogeti, Lakshminarayana; Vogeti, Subha; Yates, Karen M; Bulfer, Stacie L; Le Bourdonnec, Bertrand; Smith, Bryan D; Flynn, Daniel L.
Afiliación
  • Caldwell TM; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Kaufman MD; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Wise SC; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Mi Ahn Y; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Hood MM; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Lu WP; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Patt WC; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Samarakoon T; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Vogeti L; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Vogeti S; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Yates KM; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Bulfer SL; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Le Bourdonnec B; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Smith BD; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States.
  • Flynn DL; Deciphera Pharmaceuticals, LLC, Waltham, MA 02451, United States. Electronic address: dflynn@deciphera.com.
Bioorg Med Chem Lett ; 74: 128929, 2022 10 15.
Article en En | MEDLINE | ID: mdl-35961461
Based on the structure of an early lead identified in Deciphera's proprietary compound collection of switch control kinase inhibitors and using a combination of medicinal chemistry guided structure activity relationships and structure-based drug design, a novel series of potent acyl urea-based CSF1R inhibitors was identified displaying high selectivity for CSF1R versus the other members of the Type III receptor tyrosine kinase (RTK) family members (KIT, PDGFR-α, PDGFR-ß, and FLT3), VEGFR2 and MET. Based on in vitro biology, in vitro ADME and in vivo PK/PD studies, compound 10 was selected as an advanced lead for Deciphera's CSF1R research program.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urea / Proteínas Tirosina Quinasas Receptoras Tipo de estudio: Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urea / Proteínas Tirosina Quinasas Receptoras Tipo de estudio: Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido