Format

Send to

Choose Destination
Org Biomol Chem. 2017 Oct 18;15(40):8655-8660. doi: 10.1039/c7ob02289a.

Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety.

Author information

1
Dept of Chemistry, School of Life Sciences, University of Sussex, Falmer, BN1 9QJ, UK. j.spencer@sussex.ac.uk.
2
UK National Crystallography Service, Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, UK.
3
Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, OX3 7DQ, UK.
4
Structural Genomics Consortium, Universidade Estadual de Campinas, Campinas, SP 13083-886, Brazil.

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.

PMID:
28984325
PMCID:
PMC5708334
DOI:
10.1039/c7ob02289a
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Royal Society of Chemistry Icon for PubMed Central
Loading ...
Support Center