Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma

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dc.contributor.authorPham, TQen_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorLiu, Xen_AU
dc.contributor.authorBerghofer, PJen_AU
dc.contributor.authorBallantyne, Pen_AU
dc.contributor.authorChapman, Jen_AU
dc.contributor.authorMattner, Fen_AU
dc.contributor.authorDikic, Ben_AU
dc.contributor.authorJackson, TWen_AU
dc.contributor.authorLoc'h, Cen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.date.accessioned2014-04-16T01:45:51Zen_AU
dc.date.available2014-04-16T01:45:51Zen_AU
dc.date.issued2007-07-26en_AU
dc.date.statistics2014-04-16en_AU
dc.description.abstractThe imaging potential of a series of [123I]benzamides was studied in mice bearing B16F0 melanoma tumors. Compound [123I]25 exhibited tumor uptake >8 %ID/g at 1 h, while that of [123I]14d and [123I]25 reached a maximum of 9−12 %ID/g at 6 h. Standardized uptake values of [123I]14d were higher than 100 between 24 and 72 h after injection. In haloperidol treated animals, the tumor uptake of [123I]14d was not significantly different to controls, while significant reduction of [123I]25 uptake was observed, supporting that [123I]14d uptake relates to melanin interaction, whereas part of the mechanism of [123I]25 uptake is related to its σ1-receptor affinity. Benzamides 14d and 25, which display rapid and high tumor uptake, appear to be promising imaging agents for melanoma detection, while 14d, which displays a long lasting and high melanoma/nontarget ratio, is more suitable for evaluation as a potential radiotherapeutic. © 2007, American Chemical Society.en_AU
dc.identifier.citationPham, T. Q., Greguric, I., Liu, X., Berghofer, P., Ballantyne, P., Chapman, J., Mattner, F., Dikic, B., Jackson, T., Loc'h, C., & Katsifis, A. (2007). Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma. Journal of Medicinal Chemistry, 50(15), 3561-3572. doi:10.1021/jm0701627en_AU
dc.identifier.govdoc4536en_AU
dc.identifier.issn0022-2623en_AU
dc.identifier.issue15en_AU
dc.identifier.journaltitleJournal of Medicinal Chemistryen_AU
dc.identifier.pagination3561-3572en_AU
dc.identifier.urihttp://dx.doi.org/10.1021/jm0701627en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/5439en_AU
dc.identifier.volume50en_AU
dc.language.isoenen_AU
dc.publisherAmerican Chemical Societyen_AU
dc.subjectMelanomasen_AU
dc.subjectIn vivoen_AU
dc.subjectNeoplasmsen_AU
dc.subjectBiomedical radiographyen_AU
dc.subjectMetastasesen_AU
dc.subjectProstateen_AU
dc.titleSynthesis and evaluation of novel radioiodinated benzamides for malignant melanomaen_AU
dc.typeJournal Articleen_AU
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