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Synthesis, structural determination and photo-antiproliferative activity of new 3-pyrazolyl or -isoxazolyl substituted 4-hydroxy-2(1H)-quinolinones
Authors:Stefano Chimichi  Marco Boccalini  Francesco Dall'Acqua
Affiliation:a Dipartimento di Chimica Organica ‘U. Schiff’, via della Lastruccia 13, I-50019 Sesto F.no (Firenze), Italy
b Dipartimento di Scienze Farmaceutiche, via Marzolo 5, I-35131 Padova, Italy
c Dipartimento di Chimica e Tecnologia del Farmaco, via del Liceo 1, I-06123 Perugia, Italy
Abstract:A convenient route to new 3-quinolinonyl-pyrazoles and isoxazoles is described through cyclization of 3-[(E)-3-(dimethylamino)-2-propenoyl]-4-hydroxy-1-methyl-2(1H)-quinolinone. The phototoxicity as well as the cytotoxic activities of the title compounds are evaluated against leukemia- and adenocarcinoma-derived cell lines in comparison to the normal human keratinocytes.
Keywords:4-Hydroxy-2(1H)-quinolinones   Pyrazoles   Isoxazoles   Structural determination   15N NMR   Antitumoral compounds
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