940943-40-8Relevant articles and documents
Identification of KD5170: A novel mercaptoketone-based histone deacetylase inhibitor
Payne, Joseph E.,Bonnefous, Celine,Hassig, Christian A.,Symons, Kent T.,Guo, Xin,Nguyen, Phan-Manh,Annable, Tami,Wash, Paul L.,Hoffman, Timothy Z.,Rao, Tadimeti S.,Shiau, Andrew K.,Malecha, James W.,Noble, Stewart A.,Hager, Jeffrey H.,Smith, Nicholas D.
scheme or table, p. 6093 - 6096 (2009/07/18)
We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic activity against a range of human tumor-derived cell lines. KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or iv dose and inhibition of tumor growth following chronic dosing.
INHIBITORS OF HISTONE DEACETYLASE FOR THE TREATMENT OF DISEASE
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Page/Page column 17, (2008/06/13)
Disclosed herein are carbonyl compounds of having the structural formula: or a pharmaceutically acceptable salt, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
