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KMID : 1145520170030010044
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Journal of Radiopharmaceuticals and Molecular Probes
2017 Volume.3 No. 1 p.44 ~ p.51
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Radiosynthesis of 125I-labeled 2-cyanobenzothiazole: A new prosthetic group for efficient radioiodination reaction
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Mushtaq Sajid
Choi Dae-Seong
Jeon Jong-Ho
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Abstract
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Herein we report an efficient radiolabeling method based on a rapid condensation reaction between N-terminal cysteine and 2-cyanobenzothiazole (CBT). Radioiodination of 2-cyano-6-hydroxybenzothiazole 2 was carried out using chloramine-T to give 125I-labeled CBT ([125I]1) with a high radiochemical yield (90±6% isolated yield, n=3) and radiochemical purity (>99%). To evaluate the radiolabeling efficiency of 125I-labeled CBT, model compounds, L-cysteine and N-terminal cysteine conjugated cRGD peptide were reacted with [125I]1 under mild conditions. The radiolabeling reactions rapidly provided the 125I-labeled products [125I]5 and [125I]6 with excellent radiochemical yields and radiochemical purity. Therefore, we demonstrate that [125I]1 will be a useful prosthetic group for radioactive iodine labeling of N-terminal cysteine bearing biomolecules.
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KEYWORD
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2-Cyanobenzothiazole, Radioiodination, Bioorthogonal reaction, Biomolecules, Radiolabeling
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