Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma

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.

Keywords

Melanomas, In vivo, Neoplasms, Biomedical radiography, Metastases, Prostate

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. doi:10.1021/jm0701627