Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety.
Sansook S., Ocasio CA., Day IJ., Tizzard GJ., Coles SJ., Fedorov O., Bennett JM., Elkins JM., Spencer J.
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.