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. 2018 Feb 1;28(3):541-546.
doi: 10.1016/j.bmcl.2017.10.040. Epub 2017 Oct 20.

Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII)

Dmitry O Koltun  1 , Eric Q Parkhill  2 , Rao Kalla  2 , Thao D Perry  2 , Elfatih Elzein  2 , Xiaofen Li  2 , Scott P Simonovich  2 , Christopher Ziebenhaus  2 , Timothy R Hansen  2 , Bruno Marchand  3 , WaiLok K Hung  3 , Leanna Lagpacan  3 , Magdeleine Hung  3 , Ron G Aoyama  4 , Bernard P Murray  4 , Jason K Perry  5 , John R Somoza  5 , Armando G Villaseñor  5 , Nikos Pagratis  3 , Jeff A Zablocki  2
Affiliations

Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII)

Dmitry O Koltun et al. Bioorg Med Chem Lett. .

Abstract

We hereby disclose the discovery of inhibitors of CaMKII (7h and 7i) that are highly potent in rat ventricular myocytes, selective against hERG and other off-target kinases, while possessing good CaMKII tissue isoform selectivity (cardiac γ/δ vs. neuronal α/β). In vitro and in vivo ADME/PK studies demonstrated the suitability of these CaMKII inhibitors for PO (7h rat F = 73%) and IV pharmacological studies.

Keywords: CaMKII inhibitor; Calmodulin; Calmodulin-dependent kinase; Kinase; Protein serine/threonine kinase.

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