| Literature DB >> 21300545 |
Gabriel G Gamber1, Erik Meredith, Qingming Zhu, Wanlin Yan, Chang Rao, Michael Capparelli, Robin Burgis, Istvan Enyedy, Ji-Hu Zhang, Nicolas Soldermann, Kimberley Beattie, Olga Rozhitskaya, Keith A Koch, Nikos Pagratis, Vinayak Hosagrahara, Richard B Vega, Timothy A McKinsey, Lauren Monovich.
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.Entities:
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Year: 2011 PMID： 21300545 DOI： 10.1016/j.bmcl.2011.01.014
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823