Issue 40, 2017

Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

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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Article information

Article type
Paper
Submitted
12 Sept. 2017
Accepted
28 Sept. 2017
First published
29 Sept. 2017
This article is Open Access
Creative Commons BY license

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

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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