1.
Bioorg Med Chem Lett
; 21(5): 1447-51, 2011 Mar 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21300545
RESUMO
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.