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Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety.
Sansook, Supojjanee; Ocasio, Cory A; Day, Iain J; Tizzard, Graham J; Coles, Simon J; Fedorov, Oleg; Bennett, James M; Elkins, Jonathan M; Spencer, John.
Afiliación
  • Sansook S; Dept of Chemistry, School of Life Sciences, University of Sussex, Falmer, BN1 9QJ, UK. j.spencer@sussex.ac.uk.
  • Ocasio CA; Dept of Chemistry, School of Life Sciences, University of Sussex, Falmer, BN1 9QJ, UK. j.spencer@sussex.ac.uk.
  • Day IJ; Dept of Chemistry, School of Life Sciences, University of Sussex, Falmer, BN1 9QJ, UK. j.spencer@sussex.ac.uk.
  • Tizzard GJ; UK National Crystallography Service, Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, UK.
  • Coles SJ; UK National Crystallography Service, Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, UK.
  • Fedorov O; Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, OX3 7DQ, UK.
  • Bennett JM; Structural Genomics Consortium, Universidade Estadual de Campinas, Campinas, SP 13083-886, Brazil.
  • Elkins JM; Structural Genomics Consortium, Universidade Estadual de Campinas, Campinas, SP 13083-886, Brazil.
  • Spencer J; Dept of Chemistry, School of Life Sciences, University of Sussex, Falmer, BN1 9QJ, UK. j.spencer@sussex.ac.uk.
Org Biomol Chem ; 15(40): 8655-8660, 2017 Oct 18.
Article en En | MEDLINE | ID: mdl-28984325
ABSTRACT
A series of 3-methylidene-1H-indol-2(3H)-ones substituted with a 5- or 6-pentafluorosulfanyl group has been synthesized by a Knoevenagel condensation reaction of SF5-substituted oxindoles with a range of aldehydes. The resulting products were characterized by X-ray crystallography studies and were tested for biological activity versus a panel of cell lines and protein kinases. Some exhibited single digit nM activity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Quinasas / Compuestos de Azufre / Inhibidores de Proteínas Quinasas / Fluoruros / Indoles Límite: Humans Idioma: En Revista: Org Biomol Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Quinasas / Compuestos de Azufre / Inhibidores de Proteínas Quinasas / Fluoruros / Indoles Límite: Humans Idioma: En Revista: Org Biomol Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Reino Unido