Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
Article Details
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Pescatore G, Kinzel O, Attenni B, Cecchetti O, Fiore F, Fonsi M, Rowley M, Schultz-Fademrecht C, Serafini S, Steinkuhler C, Jones P
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32. doi: 10.1016/j.bmcl.2008.09.003. Epub 2008 Sep 6.
- PubMed ID
- 18809328 [ View in PubMed]
- Abstract
Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy and the first generation HDAC inhibitors are currently in the clinic. Herein we describe the optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Vorinostat Histone deacetylase 1 IC 50 (nM) 30 N/A N/A Details Vorinostat Histone deacetylase 2 IC 50 (nM) 82 N/A N/A Details Vorinostat Histone deacetylase 3 IC 50 (nM) 57 N/A N/A Details Vorinostat Histone deacetylase 6 IC 50 (nM) 43 N/A N/A Details