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Issue 40, 2017
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Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

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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.

Graphical abstract: Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

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Publication details

The article was received on 12 Sep 2017, accepted on 28 Sep 2017 and first published on 29 Sep 2017


Article type: Paper
DOI: 10.1039/C7OB02289A
Citation: 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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