Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

Supojjanee Sansook; Cory A. Ocasio; Iain J. Day; Graham J. Tizzard; Simon J. Coles; Oleg Fedorov; James M. Bennett; Jonathan M. Elkins; John Spencer

doi:10.1039/C7OB02289A

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Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety†

Supojjanee Sansook,‡^a Cory A. Ocasio,

^a Iain J. Day,

^a Graham J. Tizzard,

^b Simon J. Coles,

^b Oleg Fedorov,^c James M. Bennett,^d Jonathan M. Elkins

^d and John Spencer

*^a

Author affiliations

* Corresponding authors

^a Dept of Chemistry, School of Life Sciences, University of Sussex, Falmer, UK
E-mail: j.spencer@sussex.ac.uk

^b UK National Crystallography Service, Chemistry, University of Southampton, Highfield, Southampton, UK

^c Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, UK

^d Structural Genomics Consortium, Universidade Estadual de Campinas, Campinas, SP 13083-886, Brazil

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.

This article is part of the themed collection: SBQ-RSC: Celebrating UK-Brazil collaborations

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DOI: https://doi.org/10.1039/C7OB02289A
Article type: Paper
Submitted: 12 Sep 2017
Accepted: 28 Sep 2017
First published: 29 Sep 2017
This article is Open Access

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Org. Biomol. Chem., 2017,15, 8655-8660

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Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

S. Sansook, C. A. Ocasio, I. J. Day, G. J. Tizzard, S. J. Coles, O. Fedorov, J. M. Bennett, J. M. Elkins and J. Spencer, Org. Biomol. Chem., 2017, 15, 8655 DOI: 10.1039/C7OB02289A

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Organic & Biomolecular Chemistry

Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety†

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Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

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