Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety
Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety
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.
8655-8660
Sansook, Supojjanee
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Ocasio, Cory A.
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Day, Iain J.
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Tizzard, Graham J.
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Coles, Simon J.
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Fedorov, Oleg
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Bennett, James M.
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Elkins, Jonathan M.
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Spencer, John
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Sansook, Supojjanee
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Ocasio, Cory A.
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Day, Iain J.
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Tizzard, Graham J.
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Coles, Simon J.
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Fedorov, Oleg
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Bennett, James M.
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Elkins, Jonathan M.
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Spencer, John
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Sansook, Supojjanee, Ocasio, Cory A., Day, Iain J., Tizzard, Graham J., Coles, Simon J., Fedorov, Oleg, Bennett, James M., Elkins, Jonathan M. and Spencer, John
(2017)
Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety.
Organic & Biomolecular Chemistry, .
(doi:10.1039/C7OB02289A).
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.
Text
sf5 paper 21917 with table 1 added
- Accepted Manuscript
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Accepted/In Press date: 28 September 2017
e-pub ahead of print date: 29 September 2017
Identifiers
Local EPrints ID: 416349
URI: http://eprints.soton.ac.uk/id/eprint/416349
ISSN: 1477-0520
PURE UUID: 40737e83-b05f-4b46-a261-48360fc62b48
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Date deposited: 13 Dec 2017 17:30
Last modified: 16 Mar 2024 05:47
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Contributors
Author:
Supojjanee Sansook
Author:
Cory A. Ocasio
Author:
Iain J. Day
Author:
Oleg Fedorov
Author:
James M. Bennett
Author:
Jonathan M. Elkins
Author:
John Spencer
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