Abstract
(Z)-2-((1H-Indazol-3-yl)methylene)-6-methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one is a potent and selective proviral integration site in moloney murine leukemia virus kinase 1 (PIM1) inhibitor with an IC₅₀ value of 3 nM. (Z)-2-((1H-Indazol-3-yl)methylene)-6-[(11)C]methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one, a new potential PET probe for imaging of the enzyme PIM1, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-740 GBq/μmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled Boc-protected intermediate followed by a quick acidic de-protection.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Benzofurans / chemical synthesis*
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Benzofurans / chemistry*
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Carbon Isotopes / chemistry
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Fungal Proteins
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Humans
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Indazoles / chemical synthesis*
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Indazoles / chemistry
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Mice
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Mitogen-Activated Protein Kinases / antagonists & inhibitors
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Mitogen-Activated Protein Kinases / metabolism
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Neoplasms / diagnostic imaging
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Positron-Emission Tomography
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Protein Kinase Inhibitors / chemical synthesis
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
Substances
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(Z)-2-((1H-indazol-3-yl)methylene)-6-((11)C)methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one
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Benzofurans
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Carbon Isotopes
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Fungal Proteins
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Indazoles
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Piperazines
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Protein Kinase Inhibitors
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Radiopharmaceuticals
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Mitogen-Activated Protein Kinases
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Pim1 protein, Pichia pastoris
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benzofuran