PERSPECTIVE WAYS OF FINDING OF THE ANTITUMOUR PREPARATIONS BESIDES THE NEW COMPLEXES OF BACTERIAL LECTINES

Elena Welchinskaya Valeria Vilchinskaya
Pharmaceutical Department, National Medical University of A.A. Bogomolets, Kiev

By new method of synthesis between ftorotane, as fluorosubstituted syntone and 5(6)-substituted uraciles under phase-transfer conditions in alkaline medium catalysed by the 18-crown-6-complex new bis-adducts of uraciles were synthesised.

New their molecular complexes with bacterial lectines: Bacillus subtilis 668 IMV и Bacillus polymyxa 102 KGU were obtained. The main pharmacological index of the bis-adducts and their molecular complexes toxicity were obtained. The purity has been tested by method of thin-layer and gas-liquid chromatography. It was discovered that compounds, which synthesized apply to little toxic preparations: LD50 from 515 mg/kg up to 125 mg/kg. These investigations shown that molecular complexes of bis-adducts and bacterial lectines has a not hight level of toxicity - LD50 from 635 up to 125 mg/кg.

The nearest analogical compound of the bis-adducts which synthesized are antitumour preparation 5-FU. A strongly antitumour effect of compound N(1),N(1’)-(2"-bromo-2"-chloroethenyl)-bis-(5-fluorouracile) which synthesized on Lymphosarcoma Plissa tumour with growth relaxation of tumour mass 75,3% has been registered.

Therefore the bis-adducts and their molecular complexes are potential phisiological active compounds has a perspective future as potential antitumour preparations for medicines.

Key words: 5-FU, ftorotan, lectin, crown-ether, toxicity, antitumour activity.








 




Powered by Eventact EMS