Issue 3, 2012
From the journal:

MedChemComm

Developing novel non-hydroxamate histone deacetylaseinhibitors: the chelidamic warhead†‡

Sergio Valente,a   Mariarosaria Conte,b   Maria Tardugno,a   Angela Nebbioso,b   Gabriella Tinari,a   Lucia Altucci*bc  and  Antonello Mai*a  

* Corresponding authors

a Istituto Pasteur–Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro, 5, Roma, Italy
E-mail: antonello.mai@uniroma1.it
Fax: +39-0649693268
Tel: +39 0649913392

b Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. De Crecchio 7, Napoli, Italy
E-mail: lucia.altucci@unina2.it
Fax: +39 081-2144840
Tel: +39 081-5667569

c CNR-IGB, via P. Castellino, Napoli, Italy

Abstract

Herein we reported two novel series of histone deacetylaseinhibitors bearing the pyridine-2,6-dicarboxylate moiety as a zinc bindinggroup. Tested on U937 leukemia cell line at 50 μM, compounds 4a, 4c and 4d showed cell cycle block in the S phase and apoptotic induction up to 50%, whereas compound 6h was able to give granulocytic differentiation up to 40%. From these results, the chelidamic scaffold will be further investigated to find more potent compounds.

Graphical abstract: Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead

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Article information

DOI
https://doi.org/10.1039/C1MD00249J
Article type
Concise Article
Submitted
01 Oct 2011
Accepted
10 Nov 2011
First published
12 Dec 2011

Med. Chem. Commun., 2012,3, 298-304

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Developing novel non-hydroxamate histone deacetylaseinhibitors: the chelidamic warhead

S. Valente, M. Conte, M. Tardugno, A. Nebbioso, G. Tinari, L. Altucci and A. Mai, Med. Chem. Commun., 2012, 3, 298 DOI: 10.1039/C1MD00249J

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