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|Title: ||Synthesis and Evaluation of Novel Radioiodinated Benzamides for Malignant Melanoma|
|Authors: ||Pham, TQ|
|Issue Date: ||26-Jul-2007|
|Publisher: ||AMERICAN CHEMICAL SOCIETY|
|Citation: ||Pham, 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.|
|Abstract: ||The 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.|
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