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

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.

journal_name

Bioorg Med Chem Lett

authors

Wang M,Xu L,Gao M,Miller KD,Sledge GW,Zheng QH

doi

10.1016/j.bmcl.2011.01.100

subject

Has Abstract

pub_date

2011-03-15 00:00:00

pages

1649-53

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00123-5

journal_volume

21

pub_type

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