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Synthesis and Biological Activity of Some Trifluoromethyl Derivatives of 5-tert-Butyl-2-furylmethylideneanilines and Their Silyl Analogs
Authors:I Iovel  L Golomba  L Zvejniece  I Shestakova  E Lukevics
Institution:(1) Latvian Institute of Organic Synthesis, Riga, LV-1006
Abstract:We have synthesized the corresponding aldimines by condensation of 5-tert-butylfurfural and its trimethyl- and triethylsilyl analogs with 2-, 3-, and 4-trifluoromethylanilines in the presence of 4angst molecular sieves. We have studied their neurotropic and antitumor activity. The phenamine motor activity test showed that tert-butyl derivatives exhibit high efficacy and also shorten the ethanol narcosis time. Some silyl derivatives exhibit significant anti-corazole activity. The tert-butyl derivatives have high cytotoxicity toward human lung fibrosarcoma cells (the 3-trifluoromethyl-substituted derivative) and mouse hepatoma cells (the 2-trifluoromethyl-substituted derivative).
Keywords:furan Schiff's bases  silyl derivatives  trifluoromethylanilines  neurotropic activity  cytotoxicity
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