we reported two novel series of histone deacetylase inhibitors bearing the pyridine-2,6-dicarboxylate moiety as a zinc binding group. Tested on U937 leukemia cell line at 50 μM, compounds 4a, 4c and 4d showed cell cycle block in 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

Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead / Valente, Sergio; Conte, M.; Tardugno, M.; Nebbioso, A; Tinari, G.; Altucci, L.; Mai, Antonello. - In: MEDCHEMCOMM. - ISSN 2040-2503. - STAMPA. - 3:(2012), pp. 298-304. [10.1039/c1md00249j]

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

VALENTE, Sergio;MAI, Antonello
2012

Abstract

we reported two novel series of histone deacetylase inhibitors bearing the pyridine-2,6-dicarboxylate moiety as a zinc binding group. Tested on U937 leukemia cell line at 50 μM, compounds 4a, 4c and 4d showed cell cycle block in 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
2012
.
01 Pubblicazione su rivista::01a Articolo in rivista
Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead / Valente, Sergio; Conte, M.; Tardugno, M.; Nebbioso, A; Tinari, G.; Altucci, L.; Mai, Antonello. - In: MEDCHEMCOMM. - ISSN 2040-2503. - STAMPA. - 3:(2012), pp. 298-304. [10.1039/c1md00249j]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/513460
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