PET imaging using 64Cu-labeled sulfophthalocyanines: Synthesis and biodistribution

Sulfonated metallo phthalocyanines (MPcS n ) are second generation photosensitizers advanced for photodynamic therapy of various medical applications. A series of ZnPcS n was demetallated and subsequently converted to the corresponding [ 64Cu]CuPcS n in 40–50% isolated yields and >98% radiochemic...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-12, Vol.21 (24), p.7470-7473
Hauptverfasser: Ranyuk, Elena R., Cauchon, Nicole, Ali, Hasrat, Lecomte, Roger, Guérin, Brigitte, van Lier, Johan E.
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Sprache:eng
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Zusammenfassung:Sulfonated metallo phthalocyanines (MPcS n ) are second generation photosensitizers advanced for photodynamic therapy of various medical applications. A series of ZnPcS n was demetallated and subsequently converted to the corresponding [ 64Cu]CuPcS n in 40–50% isolated yields and >98% radiochemical purities. Tumor-bearing mice were injected with the 64Cu-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 [ 64Cu]CuPcS 2 and [ 64Cu]CuPcS 3C 6 (1–1.5%ID/g). The biological data suggest that PET imaging with [ 64Cu]CuPc can be used to establish structure–PDT efficacy relationships for Pc-based photosensitizers.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.09.121