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Pyrazolone-Based Zn(II) Complexes Display Antitumor Effects in Mutant p53-Carrying Cancer Cells.
Xhafa, Sonila; Di Nicola, Corrado; Tombesi, Alessia; Pettinari, Riccardo; Pettinari, Claudio; Scarpelli, Francesca; Crispini, Alessandra; La Deda, Massimo; Candreva, Angela; Garufi, Alessia; D'Orazi, Gabriella; Galindo, Agustín; Marchetti, Fabio.
Afiliação
  • Xhafa S; ChIP Research Center, School of Science and Technology, University of Camerino, via Madonna delle Carceri Camerino, 62032 Macerata, Italy.
  • Di Nicola C; ChIP Research Center, School of Science and Technology, University of Camerino, via Madonna delle Carceri Camerino, 62032 Macerata, Italy.
  • Tombesi A; ChIP Research Center, School of Pharmacy, University of Camerino, via Madonna delle Carceri Camerino, 62032 Macerata, Italy.
  • Pettinari R; ChIP Research Center, School of Pharmacy, University of Camerino, via Madonna delle Carceri Camerino, 62032 Macerata, Italy.
  • Pettinari C; ChIP Research Center, School of Pharmacy, University of Camerino, via Madonna delle Carceri Camerino, 62032 Macerata, Italy.
  • Scarpelli F; MAT-InLAB, Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, Italy.
  • Crispini A; MAT-InLAB, Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, Italy.
  • La Deda M; MAT-InLAB, Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, Italy.
  • Candreva A; MAT-InLAB, Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, Italy.
  • Garufi A; Department of Research and Advanced Technologies, IRCCS Regina Elena, National Cancer Institute, via Elio Chianesi 53, 00144 Rome, Italy.
  • D'Orazi G; Department of Research and Advanced Technologies, IRCCS Regina Elena, National Cancer Institute, via Elio Chianesi 53, 00144 Rome, Italy.
  • Galindo A; Department of Neurosciences, Imaging and Clinical Sciences, University G. D'Annunzio, via dei Vestini 31, 66013 Chieti, Italy.
  • Marchetti F; Departamento de Química Inorgánica, Facultad de Química, Universidad de Sevilla, 41012 Sevilla, Spain.
J Med Chem ; 67(17): 15676-15690, 2024 Sep 12.
Article em En | MEDLINE | ID: mdl-39221914
ABSTRACT
The synthesis and characterization of nine Schiff bases of pyrazolone ligands HLn (n = 1-9) and the corresponding zinc(II) complexes 1-9 of composition [Zn(Ln)2] (n = 1-9) are reported. The molecular structures of complexes 2, 3, 4, 8, and 9 were determined by single-crystal X-ray diffraction analysis, highlighting in all cases a distorted tetrahedral geometry around the Zn(II) ion. Density functional theory studies are performed on both the HLn ligands and the derived complexes. A mechanism of dissociation and hydrolyzation of the coordinated Schiff base ligands is suggested, confirmed experimentally by powder X-ray diffraction study and photophysical studies. Complexes 1-9 were investigated in vitro as anticancer agents, along with mutant p53 (mutp53) protein levels in human cancer cell lines carrying R175H and R273H mutp53 proteins. Only those complexes with the highest Zn(II) ion release via dissociation have shown a significant cytotoxic activity with reduction of mutp53 protein levels.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Zinco / Proteína Supressora de Tumor p53 / Pirazolonas / Complexos de Coordenação / Antineoplásicos Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Itália País de publicação: Estados Unidos
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Zinco / Proteína Supressora de Tumor p53 / Pirazolonas / Complexos de Coordenação / Antineoplásicos Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Itália País de publicação: Estados Unidos