Identification of Tri‐ and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors
Journal article published in 2010 by
Dante Rotili,
Domenico Tarantino,
Vincenzo Carafa 
,
Ester Lara,
Sarah Meade,
Giorgia Botta,
Angela Nebbioso,
Jörg Schemies,
Manfred Jung ,
Aleksey G. Kazantsev,
Manel Esteller,
Mario F. Fraga ,
Lucia Altucci,
Antonello Mai
,
Ester Lara,
Sarah Meade,
Giorgia Botta,
Angela Nebbioso,
Jörg Schemies,
Manfred Jung ,
Aleksey G. Kazantsev,
Manel Esteller,
Mario F. Fraga ,
Lucia Altucci,
Antonello Mai
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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.