ChemMedChem

Cover image for Vol. 10 Issue 6

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

April 24, 2013

VIP: tert-Butyl Carbamate Containing Histone Deacetylase Inhibitors: Apoptosis Induction, Cytodifferentiation, and Antiproliferative Activities in Cancer Cells

VIP: tert-Butyl Carbamate Containing Histone Deacetylase Inhibitors: Apoptosis Induction, Cytodifferentiation, and Antiproliferative Activities in Cancer CellsSergio Valente, Daniela Trisciuoglio, Maria Tardugno, Rosaria Benedetti, Donatella Labella, Daniela Secci, Ciro Mercurio, Roberto Boggio, Stefano Tomassi, Salvatore Di Maro, Ettore Novellino, Lucia Altucci,* Donatella Del Bufalo,* Antonello Mai*, Sandro Cosconati*

Histone deacetylase (HDAC) inhibitors are a diverse group of small-molecule drugs that induce several effects on cancer cells, including cell-cycle arrest, apoptosis, cell differentiation, autophagy, and anti-angiogenic effects. So far a large number of clinical trials with these agents have been completed and are ongoing for both hematological malignancies and solid tumors. From a collaborative research project managed by Antonello Mai, Donatella Del Bufalo, Lucia Altucci, and Sandro Cosconati, a novel class of tert-butyl-containing HDAC inhibitors has been highlighted, showing pro-apoptotic and cytodifferentiating effects in leukemia U937 cells. These inhibitors display selective inhibition at nanomolar values against HDAC6, and show sub- and low-micromolar growth inhibition against 11 different cancer cell lines. These data indicate that these molecules are worthy of further in vivo studies to validate their anticancer potential.

Received January 3, 2013; published online March 25, 2013, DOI: 10.1002/cmdc.201300005.

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