Synthesis and biological evaluation of 1,7,8,8a-tetrahydro-3H-oxazolo[3,4-a]pyrazin-6(5H)-ones as antitumoral agents |
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| Authors: | Ugo Chiacchio Vincenzina Barbera Roberta Bonfanti Gian Luigi Broggini Agata Campisi Silvia Gazzola Rosalba Parenti Giovanni Romeo |
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| Institution: | 1. Dipartimento di Scienze del Farmaco, Università di Catania, Viale A. Doria 6, 95125 Catania, Italy;2. Dipartimento di Scienza e Alta Tecnologia, Università dell’Insubria, Via Valleggio 11, 22100 Como, Italy;3. Dipartimento di Scienze Bio-Mediche, Università di Catania, Sezione di Fisiologia, Via A. Doria 6, 95125 Catania, Italy;4. Dipartimento di Scienze del Farmaco e Prodotti Per la Salute, Università di Messina, Via SS Annunziata, 98168 Messina, Italy |
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| Abstract: | A series of 1,7,8,8a-tetrahydro-3H-oxazolo3,4-a]pyrazin-6(5H)-ones has been synthesized by an intramolecular, palladium(II) catalyzed, aminooxygenation of alkenyl ureas, readily available from glycine allylamides as starting materials. Biological tests showed that the obtained compounds are endowed with an interesting antitumoral activity against two human thyroid cancer cell lines, namely FTC-133 and 8305C, by promoting the apoptotic pathway and DNA fragmentation. |
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| Keywords: | Palladium Domino reaction Bicyclic piperazinones Thyroid cancers Caspase-3 |
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