Antiproliferative Agents That Interfere with the Cell Cycle at the G(1)-->S Transition: Further Development and Characterization of a Small Library of Stilbene-Derived Compounds

Nicolo' Gebbia, Stefania Grimaudo, Rosaria Maria Pipitone, Antonietta Di Cristina, Antonietta Di Cristina, Daniela Pizzirani, Stefania Grimaudo, Maurizio Recanatini, Manlio Tolomeo, Marinella Roberti, Andrea Cavalli, Rosaria Maria Pipitone

Risultato della ricerca: Article

8 Citazioni (Scopus)

Abstract

In this continuation of our research on derivatives containing the stilbene privileged structure or that are derived from it, we report the results of further studies carried out on the previously initiated collection of compounds. We used a parallel synthetic approach to rapidly obtain small sets of compounds and started the annotation of the library in progress by calculating some physicochemical properties to be eventually correlated with biological activities. A pharmacophore for the antiproliferative activity was also built to summarize the features of the library. We evaluated the antiproliferative and pro-apoptotic activities of all compounds as well as the cell-cycle effects of some representative compounds. After in-depth investigations, 3'-phenyl- [1, 1';4', 1"]terphenyl-4,3",5"-triol showed the most interesting biological profile, as it interferes with cell-cycle progression at the G(1) -> S transition, acting on retinoblastoma phosphorylation and inducing cell differentiation.
Lingua originaleEnglish
pagine (da-a)345-355
Numero di pagine11
RivistaChemMedChem
VolumeFeb 15;3(2)
Stato di pubblicazionePublished - 2008

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Stilbenes
Libraries
Cell Cycle
Cells
Phosphorylation
Retinoblastoma
Bioactivity
Cell Differentiation
Derivatives
Research

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Organic Chemistry
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Drug Discovery
  • Pharmacology
  • Molecular Medicine

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Antiproliferative Agents That Interfere with the Cell Cycle at the G(1)-->S Transition: Further Development and Characterization of a Small Library of Stilbene-Derived Compounds. / Gebbia, Nicolo'; Grimaudo, Stefania; Pipitone, Rosaria Maria; Di Cristina, Antonietta; Di Cristina, Antonietta; Pizzirani, Daniela; Grimaudo, Stefania; Recanatini, Maurizio; Tolomeo, Manlio; Roberti, Marinella; Cavalli, Andrea; Pipitone, Rosaria Maria.

In: ChemMedChem, Vol. Feb 15;3(2), 2008, pag. 345-355.

Risultato della ricerca: Article

Gebbia, Nicolo' ; Grimaudo, Stefania ; Pipitone, Rosaria Maria ; Di Cristina, Antonietta ; Di Cristina, Antonietta ; Pizzirani, Daniela ; Grimaudo, Stefania ; Recanatini, Maurizio ; Tolomeo, Manlio ; Roberti, Marinella ; Cavalli, Andrea ; Pipitone, Rosaria Maria. / Antiproliferative Agents That Interfere with the Cell Cycle at the G(1)-->S Transition: Further Development and Characterization of a Small Library of Stilbene-Derived Compounds. In: ChemMedChem. 2008 ; Vol. Feb 15;3(2). pagg. 345-355.
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AU - Grimaudo, Stefania

AU - Pipitone, Rosaria Maria

AU - Di Cristina, Antonietta

AU - Di Cristina, Antonietta

AU - Pizzirani, Daniela

AU - Grimaudo, Stefania

AU - Recanatini, Maurizio

AU - Tolomeo, Manlio

AU - Roberti, Marinella

AU - Cavalli, Andrea

AU - Pipitone, Rosaria Maria

PY - 2008

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AB - In this continuation of our research on derivatives containing the stilbene privileged structure or that are derived from it, we report the results of further studies carried out on the previously initiated collection of compounds. We used a parallel synthetic approach to rapidly obtain small sets of compounds and started the annotation of the library in progress by calculating some physicochemical properties to be eventually correlated with biological activities. A pharmacophore for the antiproliferative activity was also built to summarize the features of the library. We evaluated the antiproliferative and pro-apoptotic activities of all compounds as well as the cell-cycle effects of some representative compounds. After in-depth investigations, 3'-phenyl- [1, 1';4', 1"]terphenyl-4,3",5"-triol showed the most interesting biological profile, as it interferes with cell-cycle progression at the G(1) -> S transition, acting on retinoblastoma phosphorylation and inducing cell differentiation.

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