A three-component reaction of phenylactylene, trifluoromethyl thianthrenium triflate (TT-CF3+OTf-) and sodium sulfinates under extremely mild conditions is developed, leading to various trifluoromethyl-substituted vinyl sulfones in moderate to good yields with excellent stereoselectivity. Additionally, elaboration of trifluoromethyl-substituted vinyl sulfone by palladium-catalyzed amination is performed. These trifluoromethyl-substituted vinyl sulfones are further evaluated for several assays against different tumor cells and the antitumor mechanism in cytotoxic autophagy induced by PI3K/Akt/mTOR signal is investigated.
Keywords: Antitumor; Cytotoxic autophagy; PI3K/Akt/mTOR; Trifluoromethylation; Vinyl sulfones.
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