THE USE OF FULLERENE IN OBTAINING BIOLOGICALLY ACTIVE COMPOUNDS BASED ON A DERIVATIVE OF VITAMIN B-12

We assumed that the introduction of a pharmacophoric fullerene derivative of the active form of vitamin B-12 into the molecule will significantly improve the efficiency of the antitumor action of the complexes. 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 C-60 derivative - ether of N-(monohydrofullerenyl)-epsilon-aminocapronic acid: HC60NH(CH2)(5)COOCH3 (II) result in the new type of mixed biologically targeted cobalamin-fullerene complexes CN-Cbl-C(O)-C60NH(CH2)(5)COOCH3 (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-B12C(O)OCH2CH2-C60NH(CH2)(5)COOCH3 (IV). For this purpose, carboxyl group (I) was modified with ethylene chlorohydrin previously. The structure of obtained substances (III) and (IV) was established by UV, IR and CD spectroscopy. The determination of the elemental composition of the samples was carried out on the basis of previously developed in the laboratory of microanalysis of the INEOS RAS different analytical methods. The content of Co and P in compounds, was determined by non-destructive X-ray fluorescence analysis (XRD) and spectrophotometry (SF) respectively and also the method of express gravimetry (EG) was chosen. For more complete information about the elemental composition of the preparations, their automatic CHN analysis was also carried out