ИСТИНА

We assumed that the introduction of a pharmacophoric fullerene derivative of the active form of vitamin B12 into the molecule will significantly improve the efficiency of the antitumor action of the complexes. To do this, first of all it was necessary to show the fundamental possibility of the synthesis of such compounds. On the first stage of the work the addition to carboxylic group of a macrocyclic cobalt complex — derivative of cobalamin e-COOH-Cbl-CN (I) the fullerene frame of the amino acid fullerene С60 derivative — ether of N-(monohydrofullerenyl)-ε-aminocapronic acid: HC60NH(CH2)5COOCH3 (II) result in the new type of mixed biologically targeted cobalamin-fullerene complexes CN-Cbl-C(O)-C60NH(CH2)5COOCH3 (III). The next derivative (IV) is obtained directly by the addition of (I) to (II), but after the additional introduction of a spacer — an ethylene bridge with the formation of the following structure: CN-Cbl-В12-C(O)OCH2CH2-C60NH(CH2)5COOCH3 (IV). The structure of obtained substances (III) and (IV) was established by UV, IR, CD spectroscopy and elemental analysis.