Novel 3-Arylideneindolin-2-ones as Inhibitors of NAD(+)-Dependent Histone Deacetylases (Sirtuins)

作者:Huber Kilian; Schemies Joerg; Uciechowska Urszula; Wagner Julia M; Rumpf Tobias; Lewrick Felicitas; Suess Regine; Sippl Wolfgang; Jung Manfred; Bracher Franz*
来源:Journal of Medicinal Chemistry, 2010, 53(3): 1383-1386.
DOI:10.1021/jm901055u

摘要

Class III historic deacetylases (sirtuins) play pivotal roles in many cellular processes. They are linked to extended lifespan and to the pathogenesis of cancer and neuronal disorders. We present novel sirtuin inhibitors based oil it 6,7-dichloro-2-oxindole scaffold with low micromolar activity. In vitro activity was rationalized by docking studies, and hyperacetylation of sirtuin targets could be demonstrated in cell culture.

  • 出版日期2010-2-11