| 摘要 |
FIELD: natural compounds, alkaloids. SUBSTANCE: invention relates to derivatives of colchicine of the formula (I) <EMI ID=0.1 HE=39 WI=47 TI=CHI> where values R1, R2, X, Me, Y are given in p. 1 of the invention claim. These compounds show antiprofilerative, antitumor and anti-inflammatory activities. Novel compounds show cytotoxicity with respect to human malignant cellular strains that is comparable with that of colchicine but show less toxicity and enhanced selectivity effect being especially to cells showing resistance to the conventional drugs. Some of the proposed compounds show the expressed activity with respect to tumor nicrosis factor and interleukin-2 and therefore they show the potent anti-inflammatory activity. They can be included into pharmaceutical compositions used for parenteral, oral and topical administration. Invention describes also the method of synthesis and a pharmaceutical composition based on compounds of the formula (I). EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 6 cl, 1 tbl, 11 ex
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