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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 (IC50) of the conjugates was evaluated against a series of human cell lines by the MTT assay. All conjugates were shown to be nontoxic (IC50 >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. [ABSTRACT FROM AUTHOR]

1-(3-Butyn-1-ylthio)-1,2-dicarba-closo-dodecaborane was synthesized by the alkylation of 1-mercapto-1,2-dicarba-closo-dodecaborane trimethylammonium salt with butyn-3-yl methanesulfonate. The deboronation reaction of this compound gave the corresponding derivative based on nido-carborane, namely, 7-(3-butyn-1-ylthio)-7,8-dicarba-undecaborate anion. 1,4-Disubstituted 1,2,3-triazoles based on closo- and nido-carboranes were synthesized by the CuI-catalyzed 1,3-dipolar [3+2] cycloaddition reaction of the acetylene derivatives of closo- and nido-carboranes with azidocholesterol. [ABSTRACT FROM AUTHOR]

The nucleophilic ring-opening reaction of tetrahydropyran derivative of the closo-dode-caborate dianion with sodium azide in the presence of tetrabutylammonium bromide led to the novel azido-derivatives of[B12H12]2−. A Cu-catalyzed 1,3-dipolar [3+2] cycloaddition reaction of the closo-dodecaborate dianion azido-derivatives with alkynyl-cholesterol led to 1,4-disubstituted 1,2,3-triazoles with the closo-dodecaborate fragment at position 1. The resulting conjugates are potentially suitable for the development of liposomal drugs to selectively deliver boron into a tumor cell for boron neutron capture therapy of cancer. [ABSTRACT FROM AUTHOR]

Owing to amphiphilicity, glycyrrhizic acid is capable of forming complexes with a variety of hydrophobic therapeutic compounds. This is accompanied by a significant decrease in the therapeutic dose of the drug. In addition, glycyrrhizic acid has a strong influence on the permeability and elasticity of cell membranes. To elucidate the molecular and cellular mechanisms of the effects observed, the effect of glycyrrhizic acid on the dynamics of lipids inside the membrane was investigated by NMR relaxation. It was found that glycyrrhizic acid can be incorporated into the membrane increasing the mobility of lipids. [ABSTRACT FROM AUTHOR]