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Synthesis and radiolabelling of Re(CO)3-β-elemene derivatives as potential therapeutic radiopharmaceuticals

✍ Scribed by Yunfeng Ren; Yanhong Sun; Kangmin Cheng; Guifeng Liu; Yumei Shen

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

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✦ Synopsis

Abstract

β‐Elemene, (1__S__, 2__S__, 4__R__)‐(−)‐(1‐methy‐1‐vinyl‐2,4‐diisopropenyl cyclohexane) is an anticancer agent from the Traditional Chinese Herb Medicinal. Three novel Re(CO)~3~‐β‐elemene derivatives including their radioactive conjugates containing N,N,N tridentate ligands and tricarbonyl rhenium (complex 12, 13, 14) were synthesized. Their structures were characterized by infrared (IR), ^1^H‐NMR and HRMS. Good radioactive yield (above 90%) and radioactive chemical purity with Re‐188 (above 95%) were obtained for all of the three derivatives (complex 15, 16, 17). The antiproliferative activity of non‐radioactive β‐elemene‐Re(CO)~3~ derivatives on Lewis lung cancer cells and HeLa cell lines were evaluated by WST‐1 methods. The result shows substantial decrease in IC~50~ values compared with the parent compound β‐elemene. The synthesis and radiosynthesis of β‐elemene tricarbonyl rhenium conjugates provide the possibility to find a new kind of potential radiopharmaceuticals on β‐elemene. Copyright © 2009 John Wiley & Sons, Ltd.

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