Synthesis of hexa aza cages, SarAr-NCS and AmBaSar and a study of their metal complexation, conjugation to nanomaterials and proteins for application in radioimaging and therapy

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dc.contributor.authorMume, Een_AU
dc.contributor.authorAsad, Aen_AU
dc.contributor.authorDi Bartolo, NMen_AU
dc.contributor.authorKong, Len_AU
dc.contributor.authorSmith, Cen_AU
dc.contributor.authorSargeson, AMen_AU
dc.contributor.authorPrice, Ren_AU
dc.date.accessioned2015-10-14T23:31:15Zen_AU
dc.date.available2015-10-14T23:31:15Zen_AU
dc.date.issued2013-07-01en_AU
dc.date.statistics2015-10-12en_AU
dc.description.abstractA novel hexa aza cage, N1-(4-isothiocyanatobenzyl)-3,6,10,13,16,19-hexaazabicyclo[6.6.6]icosane-1,8-diamine (SarAr-NCS) was synthesized in good yield and characterized by 1H NMR and electrospray mass spectrometry. A new method for the synthesis of the related N1-(4-carboxybenzyl)-3,6,10,13,16,19-hexaazabicyclo[6.6.6]icosane-1,8-diamine (AmBaSar) using the p-carboxybenzaldehyde is reported. The complexation of Cu2+, Co2+ and Zn2+ by the two ligands over a range of pHs was found to be similar to the parent derivative SarAr. SarAr-NCS was conjugated to both silica particles (≈90 nm diam.) and the model B72.3 murine antibody. The SarAr-NCSN-silica particles were radiolabeled with Cu2+ doped 64Cu and the number of ligands conjugated was calculated to be an average of 7020 ligands per particle. Conjugation of SarAr-NCS to the B72.3 antibody was optimized over a range of conditions. The SarAr-NCSN-B72.3 conjugate was stored in buffer and as a lyophilized powder at 4 °C over 38 days. Its radiolabeling efficiency, stability and immunoreactivity were maintained. The development of a high yielding synthesis of SarAr-NCS should provide an entry point for a wide range of Cu and Zn radiometal PET imaging agents and potentially radiotherapeutic agents with 67Cu. © 2013, The Royal Society of Chemistry.en_AU
dc.identifier.citationMume, E., Asad, A., Di Bartolo, N. M., Kong, L., Smith, C., Sargeson, A. M., Price, R., Smith, S. V. (2013). Synthesis of hexa aza cages, SarAr-NCS and AmBaSar and a study of their metal complexation, conjugation to nanomaterials and proteins for application in radioimaging and therapy. Dalton Transactions, 42(40), 14402-14410. doi:10.1039/c3dt51199een_AU
dc.identifier.govdoc6181en_AU
dc.identifier.issn1477-9226en_AU
dc.identifier.issue40en_AU
dc.identifier.journaltitleDalton Transactionsen_AU
dc.identifier.pagination14402-14410en_AU
dc.identifier.urihttp://dx.doi.org/10.1039/c3dt51199een_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/6332en_AU
dc.identifier.volume42en_AU
dc.language.isoenen_AU
dc.publisherRoyal Society of Chemistryen_AU
dc.subjectMass spectroscopyen_AU
dc.subjectLigandsen_AU
dc.subjectpH valueen_AU
dc.subjectRadiotherapyen_AU
dc.subjectStabilityen_AU
dc.subjectCopperen_AU
dc.titleSynthesis of hexa aza cages, SarAr-NCS and AmBaSar and a study of their metal complexation, conjugation to nanomaterials and proteins for application in radioimaging and therapyen_AU
dc.typeJournal Articleen_AU
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