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Class III histone 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 on a 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.

Original publication

DOI

10.1021/jm901055u

Type

Journal article

Journal

J Med Chem

Publication Date

11/02/2010

Volume

53

Pages

1383 - 1386

Keywords

Acetylation, Blotting, Western, Enzyme-Linked Immunosorbent Assay, Histone Deacetylase Inhibitors, Humans, Indoles, Molecular Structure, NAD, Sirtuins, Structure-Activity Relationship