Macrobicyclic cage amine ligands for copper radiopharmaceuticals: a single bivalent cage amine containing two Lys(3)-bombesin targeting peptides

Michelle Ma, Margaret Cooper, Rowena Paul, Karen Shaw, John Karas, Denis Scanlon, Jonathan White, Philip Blower, Paul Donnelly

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44 Citations (Scopus)

Abstract

The synthesis of new cage amine naacrobicyclic ligands with pendent carboxylate functional groups designed for application in copper radiopharmaceuticals is described Reaction of [Cu((NH(2))(2)sar)](2+) (sar = 3,6,10,13,16,19-hexaazabicyclo[6.6.6]icosane) with either succinic or glutaric anhydride results in selective acylation of the primary amine atoms of [Cu((NH(2))(2)sar)](2+) to give derivatives with either one or two aliphatic carboxylate functional groups separated from the cage amine framework by either a four- or five-atom linker. The Cu(II) serves to protect the secondary amine nitrogen atoms from acylation, and can be removed to give the free ligands. The newly appended carboxylate functional groups can be used as sites of attachment for cancer-targeting peptides such as Lys(3)-bombesin
Original languageEnglish
Pages (from-to)6701 - 6710
Number of pages10
JournalInorganic Chemistry
Volume50
Issue number14
DOIs
Publication statusPublished - 2011
Externally publishedYes

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