A new convenient methods for the preparation with 18-crown-6-complex as catalyst of original heterocyclic compounds (I-IV) on the base of 5-nitrouracile and fluoric containing sinton – ftorotan or 1,1-diethylcarboxy-2-chloro-2-threefluoromethylethylene were described. The method reported for the synthesis of the bis-derivative of 5-nitrouracile (scheme 1) is based on the reaction which involve elimination of fluorine hydride, formation of the intermediate 1,1-difluoro-2-bromo-2-chloroethene which react with nucleophilic molecules. The structure of synthesized compound has been confirmed by data of elemental analysis, IR- and ІН-spectra.
Molecular adduct of the bis-adduct I and antitumor bacterial lectine Bacillus polymyxa 102 KGU was obtained. It was discovered derivatives of 5-nitrouracile (I-IV) which synthesized; molecular adduct of bis-adduct I with Lectine 102 applies to a little toxic preparations: its LD50 are at the interval from 262 mg/kg to 185 mg/kg.
A strongly antitumor effect of bis-adduct I on the heterotransplantates of mans glioma cancer with percents of growth relaxation of cancer 27,48% has been discovered (the criteria are ≥25%). A strongly antitumor effect of molecular adduct (bis-adduct I– Lectine 102) on Carcinosarcoma Wokera 256 tumor with percents of growth relaxation of tumor mass 79,27% (the criteria are ≥ 50%) has been registered.
Key words: bacterial lectine, 5-nitrouracile, ftorotan, tumour.
