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Identification of Tri‐ and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors
Author(s) -
Rotili Dante,
Tarantino Domenico,
Carafa Vincenzo,
Lara Ester,
Meade Sarah,
Botta Giorgia,
Nebbioso Angela,
Schemies Jörg,
Jung Manfred,
Kazantsev Aleksey G.,
Esteller Manel,
Fraga Mario F.,
Altucci Lucia,
Mai Antonello
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000030
Subject(s) - sirtuin , hela , chemistry , sirtuin 1 , cancer cell , apoptosis , biochemistry , computational biology , nad+ kinase , cancer research , gene , biology , cancer , enzyme , genetics , in vitro , downregulation and upregulation
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.