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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.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/C7OB02289A

Authors


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Boehringer Ingelheim More from this funder
Bayer Pharma AG More from this funder
Canada Foundation for Innovation More from this funder
Ontario Genomics Institute More from this funder
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Publisher:
Royal Society of Chemistry Publisher's website
Journal:
Organic and Biomolecular Chemistry Journal website
Volume:
15
Issue:
40
Pages:
8655-8660
Publication date:
2017-09-29
Acceptance date:
2017-09-28
DOI:
EISSN:
1477-0539
ISSN:
1477-0520
Pmid:
28984325
Pubs id:
pubs:743742
UUID:
uuid:db05d24a-70af-43e1-809e-dd52f7650529
Local pid:
pubs:743742
Deposit date:
2017-11-09

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