Amino acid derivatives as histone deacetylase inhibitors
| Autor: | Thomas A. Miller, Astrid M. Kral, Richard E. Middleton, J. Paul Secrist, Jed L. Hubbs, Bethany Hughes, William K. Dahlberg, Hua Zhou, Alexander A. Szewczak, Judith C. Fleming |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
medicine.drug_class
Clinical Biochemistry Pharmaceutical Science Histone Deacetylase 1 Thiophenes Biochemistry Piperazines Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Humans Amino Acids Molecular Biology Vorinostat Histone deacetylase 5 Hydroxamic acid biology Chemistry Histone deacetylase 2 Organic Chemistry Histone deacetylase inhibitor HCT116 Cells HDAC1 Histone Deacetylase Inhibitors Enzyme inhibitor biology.protein Cancer research Molecular Medicine Histone deacetylase Drug Screening Assays Antitumor medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 18:34-38 |
| ISSN: | 0960-894X |
| Popis: | Ongoing clinical studies indicate that inhibitors of Class I and Class II histone deacetylase (HDAC) enzymes show great promise for the treatment of cancer. Zolinza® (SAHA, Zolinza®) was recently approved by the FDA for the treatment of the cutaneous manifestations of cutaneous T-cell lymphoma. As a part of an ongoing effort to identify novel small molecules to target these important enzymes, we have prepared several classes of amino acid-derived HDAC1 inhibitors. The design rationale and in vitro activity against the HDAC1 enzyme and HCT116 cell line are described in this letter. |
| Databáze: | OpenAIRE |
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