Abstract
[structure: see text] Three analogues of suberoyl anilide hydroxamic acid (SAHA) with phosphorus metal-chelating functionalities were synthesized as inhibitors of histone deacetylases (HDACs). The compounds showed weak activity for HeLa nuclear extracts (IC(50) = 0.57-6.1 mM), HDAC8 (IC(50) = 0.28-0.41 mM), and histone-deacetylase-like protein (HDLP, IC(50) = 0.33-1.9 mM), suggesting that the transition state of HDAC is not analogous to zinc proteases. Antiproliferative activity against A2780 cancer cells (IC(50) = 0.11-0.12 mM), comparable to SAHA (0.15 mM), was observed.
Original language | English |
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Pages (from-to) | 3053-3056 |
Number of pages | 0 |
Journal | Org Lett |
Volume | 5 |
Issue number | 17 |
DOIs | |
Publication status | Published - 21 Aug 2003 |
Keywords
- Antineoplastic Agents
- Bacterial Proteins
- Cell Nucleus
- Enzyme Inhibitors
- Female
- HeLa Cells
- Histone Deacetylase Inhibitors
- Humans
- Hydroxamic Acids
- Inhibitory Concentration 50
- Organophosphorus Compounds
- Ovarian Neoplasms
- Recombinant Proteins
- Tumor Cells
- Cultured
- Vorinostat