Design and synthesis of novel isoxazole-based HDAC inhibitors.

Article Details

Citation

Conti P, Tamborini L, Pinto A, Sola L, Ettari R, Mercurio C, De Micheli C

Design and synthesis of novel isoxazole-based HDAC inhibitors.

Eur J Med Chem. 2010 Sep;45(9):4331-8. doi: 10.1016/j.ejmech.2010.06.035. Epub 2010 Jun 30.

PubMed ID
20637529 [ View in PubMed
]
Abstract

A series of isoxazole-based histone deacetylase (HDAC) inhibitors structurally related to SAHA were designed and synthesized. The isoxazole moiety was inserted in the vicinity of the Zn(2+)-binding group in order to check its participation in the coordinating process.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VorinostatHistone deacetylase 1IC 50 (nM)170N/AN/ADetails
VorinostatHistone deacetylase 2IC 50 (nM)390N/AN/ADetails
VorinostatHistone deacetylase 3IC 50 (nM)200N/AN/ADetails
VorinostatHistone deacetylase 6IC 50 (nM)9.3N/AN/ADetails