Synthesis of Cobalt Bis(Dicarbollide)—Curcumin Conjugates for Potential Use in Boron Neutron Capture Therapy |
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| Authors: | Lyubov G Dezhenkova Anna A Druzina Yulia L Volodina Nadezhda V Dudarova Natalia A Nekrasova Olga B Zhidkova Mikhail A Grin Vladimir I Bregadze |
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| Institution: | 1.Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, 119021 Moscow, Russia;2.A.N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 28 Vavilov Str., 119991 Moscow, Russia; (N.V.D.); (N.A.N.); (O.B.Z.); (V.I.B.);3.Blokhin Cancer Center, 24 Kashirskoye Shosse, 115478 Moscow, Russia;4.M.V. Lomonosov Institute of Fine Chemical Technology, MIREA—Russian Technological University, 86 Vernadsky Av., 119571 Moscow, Russia; |
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| Abstract: | A series of novel cobalt bis(dicarbollide)—curcumin conjugates were synthesized. Two conjugates were obtained through the nucleophilic ring-opening reaction of the 1,4-dioxane and tetrahydropyran derivatives of cobalt bis(dicarbollide) with the OH group of curcumin, and using two equiv. of the oxonium derivatives, two other conjugates containing two cobalt bis(dicarbollide) units per molecule were obtained. In contrast to curcumin, the conjugates obtained were found to be non-cytotoxic against both tumor and normal cell lines. The analysis of the intracellular accumulation of the conjugates by flow cytometry showed that all cobalt bis(dicarbollide)—curcumin conjugates entered HCT116 colorectal carcinoma cells in a time-dependent manner. New non-cytotoxic conjugates contain a large amount of boron atoms in the biomolecule and can potentially be used for further biological research into boron neutron capture therapy (BNCT). |
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| Keywords: | curcumin cobalt bis(dicarbollide) polyhedral boron compounds cell viability intracellular accumulation |
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