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

Autor:	Istvan J. Enyedy, Wanlin Yan, Vinayak Hosagrahara, Timothy A. McKinsey, Erik Meredith, Nicolas Soldermann, Keith A. Koch, Nikos Pagratis, Qingming Zhu, Robin Burgis, Olga Rozhitskaya, Michael Paul Capparelli, Richard B. Vega, Ji-Hu Zhang, Chang Rao, Lauren G. Monovich, Kimberley Beattie, Gabriel G. Gamber
Rok vydání:	2011
Předmět:	Azoles Clinical Biochemistry Administration Oral Biological Availability Pharmaceutical Science Biochemistry Histone Deacetylases Rats Sprague-Dawley Inhibitory Concentration 50 Structure-Activity Relationship Drug Discovery Animals Structure–activity relationship Nuclear export signal Protein Kinase Inhibitors Molecular Biology Protein Kinase C chemistry.chemical_classification Histone deacetylase 5 Molecular Structure biology Kinase Chemistry Organic Chemistry Rats Enzyme Enzyme inhibitor biology.protein Molecular Medicine Histone deacetylase Signal transduction Signal Transduction
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:1447-1451
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::415a80ddabae37926dced21c7706873a https://doi.org/10.1016/j.bmcl.2011.01.014 Zobrazit plný text záznamu Full Text from ScienceDirect