(E)-β-Trifluoromethyl vinylsulfones as antitumor agents: Synthesis and biological evaluations.

Basic Information

ID: ALA5154754

Journal: Eur J Med Chem

Title: (E)-β-Trifluoromethyl vinylsulfones as antitumor agents: Synthesis and biological evaluations.

Authors: Zhang J, Wang X, Chen Q, Liu J, Zhou W, Wu J.

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.

CiteXplore: 35189568

DOI: 10.1016/j.ejmech.2022.114197

Patent ID: ┄

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