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Synthesis and evaluation of [123I]-indomethacin derivatives as COX-2 targeted imaging agents

✍ Scribed by Md. Jashim Uddin; Brenda C. Crews; Anna L. Blobaum; Philip J. Kingsley; Kebreab Ghebreselasie; Sam S. Saleh; Jeffrey A. Clanton; Ronald M. Baldwin; Lawrence J. Marnett

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
243 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A novel series of iodinated indomethacin derivatives was synthesized, and evaluated as selective inhibitors of COX‐2. Two candidate compounds N‐(p‐iodobenzyl)‐2‐(1‐(p‐chlorobenzoyl)‐5‐methoxy‐2‐methyl‐1__H__‐indol‐3‐yl)acetamide (3) and 1‐(p‐iodobenzyl)‐5‐methoxy‐2‐methyl‐3‐indoleacetic acid (9) possessed optimum properties suitable for potential in vivo imaging. Arylstannane precursors for radioiododestannylation were synthesized in 70–85% yield from the iodo compounds by reaction with hexabutylditin and tetrakis(triphenylphosphine)palladium(0) in refluxing dioxane. Radioiododestannylation was conducted by reaction with carrier‐added Na[^123^I] in the presence of Chloramine‐T in an EtOAc/H~2~O binary system under acidic conditions (pH 3.5), allowing direct isolation of the labeled products by separation of the organic phase. Radioiodinated products [^123^I]3 and [^123^I]9 were recovered in a decay‐corrected radiochemical yield of 86–87% and radiochemical purity of 98–99%. Copyright © 2009 John Wiley & Sons, Ltd.

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