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.

PIZZIRANI D, ROBERTI M, CAVALLI A, GRIMAUDO S, DI CRISTINA A, PIPITONE MR, et al. (2008). 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. CHEMMEDCHEM, Feb 15;3(2)(2), 345-355.

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

GRIMAUDO, Stefania;DI CRISTINA, Antonietta;PIPITONE, Rosaria Maria;GEBBIA, Nicolo';
2008-01-01

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.
2008
PIZZIRANI D, ROBERTI M, CAVALLI A, GRIMAUDO S, DI CRISTINA A, PIPITONE MR, et al. (2008). 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. CHEMMEDCHEM, Feb 15;3(2)(2), 345-355.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/34023
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