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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.

SUBMITTER: Sansook S

PROVIDER: S-EPMC5708334 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety.

Sansook Supojjanee S Ocasio Cory A CA Day Iain J IJ Tizzard Graham J GJ Coles Simon J SJ Fedorov Oleg O Bennett James M JM Elkins Jonathan M JM Spencer John J

Organic & biomolecular chemistry 20171001 40

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 SF<sub>5</sub>-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. ...[more]

PMID: 28984325

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