149648-49-7Relevant academic research and scientific papers
Inhibitors of histone deacetylase suppress the growth of MCF-7 breast cancer cells
Schmidt, Kathrin,Gust, Ronald,Jung, Manfred
, p. 353 - 357 (1999)
Inhibitors of histone deacetylase are attracting increasing interest due to their influence on transcription, differentiation, and apoptosis. We have investigated two synthetic inhibitors 3 and 4 of histone deacetylase and the natural product inhibitor tr
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation
Ghosh, Balaram,Zhao, Wen-Ning,Reis, Surya A.,Patnaik, Debasis,Fass, Daniel M.,Tsai, Li-Huei,Mazitschek, Ralph,Haggarty, Stephen J.
supporting information, p. 1265 - 1271 (2016/02/23)
Targeting chromatin-mediated epigenetic regulation has emerged as a potential avenue for developing novel therapeutics for a wide range of central nervous system disorders, including cognitive disorders and depression. Histone deacetylase (HDAC) inhibitor
HISTONE DEACETYLASE INHIBITORS
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Page/Page column 47; fig. 13, (2010/04/23)
In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are p
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: In vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in friend leukemic cells
Wittich, Sybille,Scherf, Hans,Xie, Changping,Brosch, Gerald,Loidl, Peter,Gerh?user, Clarissa,Jung, Manfred
, p. 3296 - 3309 (2007/10/03)
Inhibitors of histone deacetylases (HDACs) are a new class of anticancer agents that affect gene regulation. We had previously reported the first simple synthetic HDAC inhibitors with in vitro activity at submicromolar concentrations. Here, we present structure-activity data on modifications of a phenylalanine-containing lead compound including amino acid amides as well as variations of the amino acid part. The compounds were tested for inhibition of maize HD-2, rat liver HDAC, and for the induction of terminal cell differentiation and inhibition of proliferation in Friend leukemic cells. In the amide series, in vitro inhibition was potentiated up to 15-fold, but the potential to induce cell differentiation decreased. Interestingly, an HDAC class selectivity was indicated among some of these amides. In the amino acid methyl ester series, a biphenylalanine derivative was identified as a good enzyme inhibitor, which blocks proliferation in the submicromolar range and is also a potent inducer of terminal cell differentiation.
