DERIVATIVES OF COLCHICINE, METHODS OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITIONS BASED ON THEREOF Russian patent published in 2002 - IPC

FIELD: organic chemistry of natural compounds, alkaloids. SUBSTANCE: invention relates to derivatives of colchicine of the formula (I) where R means methoxy-group or methylthio-group; R₁ means linear or branched C₁-C₆-alkyl under condition that if R means methoxy- group then R₁ can not mean methyl group. Invention relates to compounds of the formula (II) where R means methylthio- group; R₁ means linear or branched C₁-C₆-alkyl. Compounds of the formula (I) are synthesized by interaction of N- desacetylthiocolchicine or N-desacetyl-colchicine with 1,8-diazabicyclo[5,4,0]undec-7-ene. Compounds of the formula (II) are synthesized by interaction of N-desacetylthiocolchicine with 3,5-di-tert.-butyl-1,2- -benzoquinone. Compounds of the formulas (I) and (II) show antitumor and antiproliferative activity that ensures to use their in pharmaceutical composition as an active component useful for topical using. EFFECT: improved method of synthesis, valuable medicinal properties. 13 cl, 2 tbl, 8 ex