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Bioorg Med Chem Lett. 2011 Mar 15;21(6):1649-53. doi: 10.1016/j.bmcl.2011.01.100. Epub 2011 Jan 31.

[11C]enzastaurin, the first design and radiosynthesis of a new potential PET agent for imaging of protein kinase C.

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  • 1Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA.

Abstract

Enzastaurin (LY317615) is a potent and selective protein kinase C (PKC) inhibitor with an IC(50) value of ∼6 nM. [(11)C]Enzastaurin (3-(1-[(11)C]methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of PKC, was first designed and synthesized in 20-25% decay corrected radiochemical yield and 370-555 GBq/μmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled maleic anhydride intermediate followed by the conversion to maleimide.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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