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Synthesis and antiproliferative activities of two new analogs of tetrazepinones

  • Autori: Raimondi, M.; Maggio, B.; Raffa, D.; Plescia, F.; Grimaudo, S.; Tolomeo, M.; Daidone, G.
  • Anno di pubblicazione: 2016
  • Tipologia: Proceedings (TIPOLOGIA NON ATTIVA)


Based on the encouraging results, we report the multistep synthesis and the biologicalo results of two new analogs of tetrazepinones: the 3,5-dimethyl-6-phenyl-8-(trifluoromethyl-5,6-dihydropyrazo1o[3-4-f]1,2,35)tetrazepin-4(3H)-one and the 3-(2-chloroethyl)-5-methyl-6-phenyl-8-(trifluoromethyl-5,6-dihydropyrazo1o[3-4-f]1,2,35)tetrazepin-4(3H)-one. Both compounds showed a pro-apoptotic activity against HL60 and K562 resistant cell lines. Flow cytometry studies carried out 0n K562 cells allowed to establish that the methyl derivative induces G0-G1, phase arrest followed by apoptosis, whereas the chloroethyl derivative is a not phase-specific agent.