Synthesis and radiolabelling of Re(CO)3-β-elemene derivatives as potential therapeutic radiopharmaceuticals
| Autor: | Guifeng Liu, Yu-Mei Shen, Yanhong Sun, Yunfeng Ren, Kangmin Cheng |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
biology
Tertiary amine Stereochemistry Organic Chemistry Radiosynthesis chemistry.chemical_element Rhenium biology.organism_classification Biochemistry Chemical synthesis Medicinal chemistry Analytical Chemistry HeLa chemistry.chemical_compound chemistry Drug Discovery Lipophilicity Radiology Nuclear Medicine and imaging Elemene Spectroscopy Conjugate |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 52:139-145 |
| ISSN: | 1099-1344 0362-4803 |
| Popis: | β-Elemene, (1S, 2S, 4R)-(−)-(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), 1H-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 IC50 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. |
| Databáze: | OpenAIRE |
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