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

Gamber, Gabriel and Meredith, Erik and Zhu, Qingming and Yan, Wanlin and Rao, Chang and Capparelli, Michael and Burgis, Robin and Enyedy, Istvan and Zhang, Ji and Soldermann, Nicolas and Beattie, Kimberley and Rozhitskaya, Olga and Koch, Keith and Pagratis, Nikos and Hosagrahara, Vinayak and Vega, Richard and 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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