Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366055 | Bioorganic & Medicinal Chemistry Letters | 2007 | 7 Pages |
Inhibition of histone deacetylases class I/II enzymes is a new, promising approach for cancer therapy. In the present study, we disclose a new structural class of HDAC inhibitors with the trithiocarbonate motif. A clear structure–activity-relationship was obtained for the cap-linker motif and the putative Zn2+ complexing head group. Selected analogs display potent inhibition of HDAC enzymatic activity and a cellular potency comparable to that of suberoylanilide hydroxamic acid (SAHA), recently approved for treatment of patients with advanced cutaneous T-cell lymphoma.
Graphical abstractTrithiocarbonates are described as a new class of head groups for HDAC inhibition with biochemical and cellular activity.Figure optionsDownload full-size imageDownload as PowerPoint slide