(Chemical Equation Presented) Sirtuins are deacetylase proteins that regulate transcription, genome maintenance, longevity, and metabolism. Eight compounds were identified as a novel class of sirtuin inhibitors, with 5, 7, and 9 being the most effective as SIRT1-selective inhibitors. In U937 cells 5 induced apoptosis and displayed antiproliferative effects in Raji, DLD1, and HeLa cancer cells, suggesting potential utility in cancer treatment. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

Identification of Tri- and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors / Rotili, Dante; Tarantino, Domenico; Vincenzo, Carafa; Ester, Lara; Sarah, Meade; Giorgia, Botta; Angela, Nebbioso; Jorg, Schemies; Manfred, Jung; Aleksey g, Kazantsev; Manel, Esteller; Mario f, Fraga; Lucia, Altucci; Mai, Antonello. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 5:5(2010), pp. 674-677. [10.1002/cmdc.201000030]

Identification of Tri- and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors

ROTILI, Dante;TARANTINO, DOMENICO;MAI, Antonello
2010

Abstract

(Chemical Equation Presented) Sirtuins are deacetylase proteins that regulate transcription, genome maintenance, longevity, and metabolism. Eight compounds were identified as a novel class of sirtuin inhibitors, with 5, 7, and 9 being the most effective as SIRT1-selective inhibitors. In U937 cells 5 induced apoptosis and displayed antiproliferative effects in Raji, DLD1, and HeLa cancer cells, suggesting potential utility in cancer treatment. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.
2010
antiproliferation; apoptosis; diazabenzoanthracene; inhibitors; sirtuins
01 Pubblicazione su rivista::01a Articolo in rivista
Identification of Tri- and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors / Rotili, Dante; Tarantino, Domenico; Vincenzo, Carafa; Ester, Lara; Sarah, Meade; Giorgia, Botta; Angela, Nebbioso; Jorg, Schemies; Manfred, Jung; Aleksey g, Kazantsev; Manel, Esteller; Mario f, Fraga; Lucia, Altucci; Mai, Antonello. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 5:5(2010), pp. 674-677. [10.1002/cmdc.201000030]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/456116
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