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Synthesis and radiolabelling of Re(CO) 3 ‐ β ‐elemene derivatives as potential therapeutic radiopharmaceuticals
Author(s) -
Ren Yunfeng,
Sun Yanhong,
Cheng Kangmin,
Liu Guifeng,
Shen Yumei
Publication year - 2009
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1580
Subject(s) - chemistry , elemene , rhenium , radiosynthesis , hela , combinatorial chemistry , yield (engineering) , radiochemistry , stereochemistry , organic chemistry , in vitro , in vivo , biochemistry , apoptosis , microbiology and biotechnology , materials science , metallurgy , biology
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.