Potent histone deacetylase inhibitors: N-hydroxybenzamides with antitumor activities
| Autor: | Taishi Maeda, Yasuo Nagaoka, Mineko Kurotaki, Chieko Seno, Sakiko Maruyama, Hiroshi Kuwajima, Shinichi Uesato |
|---|---|
| Rok vydání: | 2004 |
| Předmět: |
medicine.drug_class
Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry chemistry.chemical_compound Mice In vivo Cell Line Tumor Drug Discovery medicine Animals Humans Enzyme Inhibitors Cytotoxicity Molecular Biology chemistry.chemical_classification Hydroxamic acid biology Chemistry Organic Chemistry Histone deacetylase inhibitor Xenograft Model Antitumor Assays In vitro Histone Deacetylase Inhibitors Enzyme Enzyme inhibitor Benzamides biology.protein Molecular Medicine Female Histone deacetylase Drug Screening Assays Antitumor |
| Zdroj: | Bioorganicmedicinal chemistry. 12(16) |
| ISSN: | 0968-0896 |
| Popis: | The screening tests of N-hydroxybenzamides for their HDAC-inhibitory activities led to the discovery of the promising compounds with a 2-naphthylcarbonyl group and with a 1,4-biphenylcarbonyl group. These compounds were further modified to optimize their physico-chemical profile. As a result, the inhibitor with a 6-amino-2-naphthylcarbonyl was obtained, which showed not only promising growth inhibitions against a panel of tumor cells, but also an improved water solubility. It exhibited the maximal 185% of survival rate (%T/C) in a in vivo experiment with P388 cell-inoculated mice. |
| Databáze: | OpenAIRE |
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