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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.

Original publication

DOI

10.1039/c7ob02289a

Type

Journal article

Journal

Org Biomol Chem

Publication Date

18/10/2017

Volume

15

Pages

8655 - 8660

Keywords

Cell Line, Cell Proliferation, Crystallography, X-Ray, Dose-Response Relationship, Drug, Fluorides, Humans, Indoles, Models, Molecular, Molecular Structure, Oxindoles, Protein Kinase Inhibitors, Protein Kinases, Structure-Activity Relationship, Sulfur Compounds