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Preliminary Studies of 3,5-Diarylazoles as Novel and Selective Inhibitors of Protein Kinase D

Gamber, Gabriel, Meredith, Erik, Zhu, Qingming, Yan, Wanlin, Rao, Chang, Capparelli, Michael, Burgis, Robin, Enyedy, Istvan, Zhang, Ji, Soldermann, Nicolas, Beattie, Kimberley, Rozhitskaya, Olga, Koch, Keith, Pagratis, Nikos, Hosagrahara, Vinayak, Vega, Richard, McKinsey, Timothy and Monovich, Lauren (2010) Preliminary Studies of 3,5-Diarylazoles as Novel and Selective Inhibitors of Protein Kinase D. Bioorganic and Medicinal Chemistry Letters, 21 (5). pp. 1447-1451. ISSN 0960-894X

Abstract

Preliminary studies of the SAR of novel 3,5-diarylazole inhibitors of Protein Kinase D (PKD) are reported. Notably, compounds bearing an α-aminonitrile moiety have been found to be active in cellular assays of HDAC5 nuclear localization, orally biovailable, and highly selective versus a panel of additional putative histone deacetylase (HDAC) kinases, providing potential tools for the further study of PKD / HDAC5 signaling

Item Type: Article
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16
URI: https://oak.novartis.com/id/eprint/2142

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