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 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2011.09.121 |