Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity

Rosaria Maria Pipitone, Stefania Grimaudo, Federico Falchi, Cristina Ianni, Elisa Giacomini, Alfonso Ciotta, Lucia Altucci, Maurizio Recanatini, Marinella Roberti, Angela Nebbioso

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11 Citazioni (Scopus)

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.
Lingua originaleEnglish
pagine (da-a)973-978
Numero di pagine6
RivistaACS Medicinal Chemistry Letters
VolumeJul8;5(9)
Stato di pubblicazionePublished - 2014

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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    Pipitone, R. M., Grimaudo, S., Falchi, F., Ianni, C., Giacomini, E., Ciotta, A., Altucci, L., Recanatini, M., Roberti, M., & Nebbioso, A. (2014). Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity. ACS Medicinal Chemistry Letters, Jul8;5(9), 973-978.