Synthesis, Radiolabelling and Preliminary Bioactivity of β-Elemene-TEG-Re(CO)3 Complex

Chem. J. Chinese Universities

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Synthesis, Radiolabelling and Preliminary Bioactivity of β-Elemene-TEG-Re(CO)₃ Complex

REN Yun-Feng^1,2, LIU Gui-Feng^1,2, SUN Yan-Hong¹, SHEN Yu-Mei¹

1. Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China;
2. Graduate School of the Chinese Academy of Sciences, Beijing 100049, China

Received:2008-01-29 Revised:1900-01-01 Online:2008-09-10 Published:2008-09-10
Contact: SHEN Yu-Mei

Abstract

Abstract: β-Elemene, (5S,7R,10S)-(-)-(1-methyl-1-vinyl-2,4-diisopropenyl-cyclohexane) is an anti-cancer agent from the Traditional Chinese Herb Medicinal. Accordingly, we synthesized β-Elemene-TEG-Re(CO)₃ complexe and evaluated it as a potential radiopharmaceuticals. The structures and properties of the intermediate were indentified via IR, ¹H NMR and HRMS. Good radioactive yield(above 90%) and radioactive chemical purity with Re-188(above 97%) were obtained. The antiproliferative activity of non-radioactive β-Elemene-TEG-Re(CO)₃ derivatives on LLC and Hela cell lines were evaluated by WST-1 methods. The result shows a substantial decrease of IC₅₀ values compared with that of the parent compound β-elemene.

Key words: β-Elemene, Re(CO)₃, Re-188, Radiolabelling, Bioactivity

CLC Number:

O621.3⁺5

TrendMD:

REN Yun-Feng^1,2, LIU Gui-Feng^1,2, SUN Yan-Hong¹, SHEN Yu-Mei¹

. Synthesis, Radiolabelling and Preliminary Bioactivity of β-Elemene-TEG-Re(CO)₃ Complex[J]. Chem. J. Chinese Universities, doi: .

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Synthesis, Radiolabelling and Preliminary Bioactivity of β-Elemene-TEG-Re(CO)₃ Complex

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