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Bioorg Med Chem Lett. 2011 Mar 1;21(5):1447-51. doi: 10.1016/j.bmcl.2011.01.014. Epub 2011 Jan 11.

3,5-diarylazoles as novel and selective inhibitors of protein kinase D.

Author information

1
Novartis Institutes for BioMedical Research, Cambridge, MA 02139, USA. gabriel.gamber@novartis.com

Abstract

The synthesis and preliminary studies of the SAR of novel 3,5-diarylazole inhibitors of Protein Kinase D (PKD) are reported. Notably, optimized compounds in this class have been found to be active in cellular assays of phosphorylation-dependant HDAC5 nuclear export, orally bioavailable, and highly selective versus a panel of additional putative histone deacetylase (HDAC) kinases. Therefore these compounds could provide attractive tools for the further study of PKD/HDAC5 signaling.

PMID:
21300545
DOI:
10.1016/j.bmcl.2011.01.014
[Indexed for MEDLINE]

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