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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
(E)-β-Trifluoromethyl vinylsulfones as antitumor agents: Synthesis and biological evaluations
Jun Zhang1, Xuefeng Wang2, Qi Chen1
1Taizhou Central Hospital (Taizhou University Hospital) & School of Pharmaceutical and Materials Engineering, Taizhou University, 999 Donghai Avenue, Taizhou, 318000, China.
Abstract:
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.
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