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  • Title: Trithiocarbonates: exploration of a new head group for HDAC inhibitors.
    Author: Dehmel F, Ciossek T, Maier T, Weinbrenner S, Schmidt B, Zoche M, Beckers T.
    Journal: Bioorg Med Chem Lett; 2007 Sep 01; 17(17):4746-52. PubMed ID: 17606370.
    Abstract:
    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 Zn(2+) 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.
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