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Eur J Med Chem. 2013;70:857-63. doi: 10.1016/j.ejmech.2013.09.057. Epub 2013 Oct 12.

Azetidinone-retinoid hybrids: synthesis and differentiative effects.

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  • 1Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.

Abstract

As a part of a systematic investigation on the synthesis and biological activities of new β-lactam compounds, we examined β-lactam candidates 1, 2E and 2Z and their ability to induce cell proliferation or differentiation. Azetidinone 1 was chosen for its activity (previously evaluated) as selective HDAC8 inhibitor, whereas β-lactams 2E and 2Z were designed to have a hybrid retinoid-azetidinone structure, de novo synthesized and fully characterized. Biological activities were determined in cellular assays on neuroblastoma cells SH-SY5Y. Azetidinone 1, 2E and 2Z led to a moderate effect in decreasing SH-SY5Y cell proliferation and β-lactams 2E and 2Z induced an early stage differentiation. The present results uncovered a new role of specifically designed β-lactam compounds in epigenetic regulation.

Copyright © 2013 Elsevier Masson SAS. All rights reserved.

KEYWORDS:

Cell differentiation; Epigenetic regulation; HDAC inhibitors; Retinoids; Synthesis; β-Lactams

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