Trithiocarbonates—exploration of a new head group for HDAC inhibitors

F Dehmel, T Ciossek, T Maier, S Weinbrenner…

文献索引：Dehmel, Florian; Ciossek, Thomas; Maier, Thomas; Weinbrenner, Steffen; Schmidt, Beate; Zoche, Martin; Beckers, Thomas Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 17 p. 4746 - 4752

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被引用次数: 32

摘要

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 ...