1262844-65-4Relevant academic research and scientific papers
3,5-Diarylazoles as novel and selective inhibitors of protein kinase D
Gamber, Gabriel G.,Meredith, Erik,Zhu, Qingming,Yan, Wanlin,Rao, Chang,Capparelli, Michael,Burgis, Robin,Enyedy, Istvan,Zhang, Ji-Hu,Soldermann, Nicolas,Beattie, Kimberley,Rozhitskaya, Olga,Koch, Keith A.,Pagratis, Nikos,Hosagrahara, Vinayak,Vega, Richard B.,McKinsey, Timothy A.,Monovich, Lauren
, p. 1447 - 1451 (2011)
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.
ARYLPYRAZOLES AND ARYLISOXAZOLES AND THEIR USE AS PKD MODULATORS
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Page/Page column 69, (2011/02/24)
The present invention provides novel organic compounds of formula (I) or (Ia): which may be inhibitors of a selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example PKD-1/2/3, inhibitors of histone deacetylase (HDA
