2. Academic Validation
  3. Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity

Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity

  • ACS Med Chem Lett. 2014 Jul 8;5(9):973-8. doi: 10.1021/ml5000959.
Elisa Giacomini 1,  Angela Nebbioso 2,  Alfonso Ciotta 2,  Cristina Ianni 3,  Federico Falchi 1,  Marinella Roberti 3,  Manlio Tolomeo 4,  Stefania Grimaudo 5,  Antonietta Di Cristina 5,  Rosaria Maria Pipitone 5,  Lucia Altucci 6,  Maurizio Recanatini 3
Affiliations

Affiliations

  • 1 Department of Pharmacy and Biotechnology, University of Bologna , Via Belmeloro 6, 40126 Bologna, Italy ; Department of Drug Discovery and Development, Italian Institute of Technology , Via Morego 30, 16163 Genova, Italy.
  • 2 Department of Biochemistry, Biophysics and General Pathology, Second University of Naples , Vico L. De Crecchio 7, 80138 Naples, Italy.
  • 3 Department of Pharmacy and Biotechnology, University of Bologna , Via Belmeloro 6, 40126 Bologna, Italy.
  • 4 Interdepartmental Center of Research in Clinical Oncology and Department of Infectious Diseases, University of Palermo , Via del Vespro 129, 90127 Palermo, Italy.
  • 5 DiBiMIS, Laboratory of Molecular Pathology, Institute of Gastroenterology, University of Palermo , Piazza delle Cliniche 2, 90127 Palermo, Italy.
  • 6 Department of Biochemistry, Biophysics and General Pathology, Second University of Naples , Vico L. De Crecchio 7, 80138 Naples, Italy ; Institute of Genetics and Biophysics, IGB, Via Pietro Castellino 111, 80131 Naples, Italy.
PMID: 25221651 DOI: 10.1021/ml5000959
Abstract

Given our interest in finding potential antitumor agents and in view of the multifactorial mechanistic nature of Cancer, in the present work, taking advantage of the multifunctional ligands approach, new chimeric molecules were designed and synthesized by combining in single chemical entities structural features of SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained by us and endowed with antiproliferative and pro-apoptotic activity. The new chimeric derivatives were characterized with respect to their cytotoxic activity and their effects on cell cycle progression on different tumor cell lines, as well as their HDACs inhibition. Among the Other, trans -6 showed the most interesting biological profile, as it exhibited a strong pro-apoptotic activity in tumor cell lines in comparison with both of its parent compounds and a marked HDAC inhibition.

Keywords

HDAC inhibition; Multifunctional ligands; antiproliferative activity; chimeric compound; stilbene.

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