Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX
The inhibition of HDAC (histone deacetylase) activity by specific inhibitors induces growth arrest, differentiation and apoptosis of transformed or several cancer cells. Some of these inhibitors are in clinical trial at phase I or phase II. The discovery and development of specific HDAC inhibitors a...
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| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Wiley
2011-01-01
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| Series: | E-Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2011/572546 |
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| _version_ | 1832567244654116864 |
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| author | Lynda Ekou Tchirioua Ekou Isabelle Opalinski Jean Pierre Gesson |
| author_facet | Lynda Ekou Tchirioua Ekou Isabelle Opalinski Jean Pierre Gesson |
| author_sort | Lynda Ekou |
| collection | DOAJ |
| description | The inhibition of HDAC (histone deacetylase) activity by specific inhibitors induces growth arrest, differentiation and apoptosis of transformed or several cancer cells. Some of these inhibitors are in clinical trial at phase I or phase II. The discovery and development of specific HDAC inhibitors are helpful for cancer therapy. In this paper we describe the synthesis of simple inhibitor B hybrid analogue suberoylanilide hydroxamic acid (SAHA), trapoxin B (TPX B) in as little as five steps. This compound is interesting lead for the design of potent inhibitors of histone deacetylase. |
| format | Article |
| id | doaj-art-995007e3bd534c1cb5cd67c62251c4ac |
| institution | Kabale University |
| issn | 0973-4945 2090-9810 |
| language | English |
| publishDate | 2011-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | E-Journal of Chemistry |
| spelling | doaj-art-995007e3bd534c1cb5cd67c62251c4ac2025-02-03T01:01:59ZengWileyE-Journal of Chemistry0973-49452090-98102011-01-018S1S79S8410.1155/2011/572546Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPXLynda Ekou0Tchirioua Ekou1Isabelle Opalinski2Jean Pierre Gesson3Université d'Abobo-Adjamé, Laboratoire de Thermodynamique et de Physico-Chimie du Milieu, 02 BP 801 Abidjan 02, Cote D'IvoireUniversité d'Abobo-Adjamé, Laboratoire de Thermodynamique et de Physico-Chimie du Milieu, 02 BP 801 Abidjan 02, Cote D'IvoireUniversité de Poitiers, UMR-CNRS-6514, Laboratoire de Synthèse et Réactivité des Substances Naturelles, 40 Avenue du Recteur Pineau, Poitiers Cedex-86022, FranceUniversité de Poitiers, UMR-CNRS-6514, Laboratoire de Synthèse et Réactivité des Substances Naturelles, 40 Avenue du Recteur Pineau, Poitiers Cedex-86022, FranceThe inhibition of HDAC (histone deacetylase) activity by specific inhibitors induces growth arrest, differentiation and apoptosis of transformed or several cancer cells. Some of these inhibitors are in clinical trial at phase I or phase II. The discovery and development of specific HDAC inhibitors are helpful for cancer therapy. In this paper we describe the synthesis of simple inhibitor B hybrid analogue suberoylanilide hydroxamic acid (SAHA), trapoxin B (TPX B) in as little as five steps. This compound is interesting lead for the design of potent inhibitors of histone deacetylase.http://dx.doi.org/10.1155/2011/572546 |
| spellingShingle | Lynda Ekou Tchirioua Ekou Isabelle Opalinski Jean Pierre Gesson Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX E-Journal of Chemistry |
| title | Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX |
| title_full | Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX |
| title_fullStr | Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX |
| title_full_unstemmed | Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX |
| title_short | Histone Deacetylase Inhibitors: Synthesis of Tetrapeptide Analogue SAHA/TPX |
| title_sort | histone deacetylase inhibitors synthesis of tetrapeptide analogue saha tpx |
| url | http://dx.doi.org/10.1155/2011/572546 |
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