Cobalt and iron bis(dicarbollide) conjugates with cholesterol: synthesis and evaluation of antiproliferative activity

K. E. Erdelyi, A. A. Antonets, O. B. Zhidkova, A. A. Druzina, A. A. Nazarov,S. V. Timofeev, I. B. Sivaev, V. I. Bregadze

RUSSIAN CHEMICAL BULLETIN(2023)

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摘要
Boron-containing conjugates of cholesterol were synthesized by the copper( i )-catalyzed 1,3-dipolar [3+2] cycloaddition reactions of cobalt and iron bis(dicarbollide) azide derivatives with alkynyl cholesterol. The antiproliferative activity (IC 50 ) of the conjugates was evaluated against a series of human cell lines by the MTT assay. All conjugates were shown to be nontoxic (IC 50 >200 µmol L −1 ) and to be applicable for the preparation of boron-containing liposomes as potential drugs for boron-neutron capture therapy (BNCT) of cancer.
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关键词
cobalt/iron bis(dicarbollide),cholesterol,lipids,click reaction,boron neutron capture therapy
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