Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.

Article Details

Citation
Copy to clipboard

Tapadar S, He R, Luchini DN, Billadeau DD, Kozikowski AP

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3023-6. doi: 10.1016/j.bmcl.2009.04.058. Epub 2009 Apr 20.

PubMed ID
19419863 [ View in PubMed
]
Abstract

A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micro molar inhibitory activity against five pancreatic cancer cell lines.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VorinostatHistone deacetylase 1IC 50 (nM)96N/AN/ADetails
VorinostatHistone deacetylase 2IC 50 (nM)282N/AN/ADetails
VorinostatHistone deacetylase 3IC 50 (nM)17N/AN/ADetails
VorinostatHistone deacetylase 6IC 50 (nM)14N/AN/ADetails