Pet Imaging Using Cu-64-Labeled Sulfophthalocyanines: Synthesis And Biodistribution

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2011)

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Abstract
Sulfonated metallo phthalocyanines (MPcSn) are second generation photosensitizers advanced for photodynamic therapy of various medical applications. A series of ZnPcSn was demetallated and subsequently converted to the corresponding [Cu-64]CuPcSn in 40-50% isolated yields and >98% radiochemical purities. Tumor-bearing mice were injected with the Cu-64-labeled products and subjected to 3-h dynamic PET imaging studies. Biodistribution patterns showed characteristic differences between the various derivatives. Tumor uptake was detected only for the amphiphilic derivatives [Cu-64]CuPcS2 and [Cu-64]CuPcS3C6 (1-1.5% ID/g). The biological data suggest that PET imaging with [Cu-64]CuPc can be used to establish structure-PDT efficacy relationships for Pc-based photosensitizers. (C) 2011 Elsevier Ltd. All rights reserved.
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Key words
Phthalocyanine, Cu-64, PDT, PET-imaging
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