6,9-BIS-(AMINOSUBSTITUTED)-BENZO[G]ISOQUINOLINE-5,10-DIONES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION ON THEIR BASIS, A METHOD OF TUMOR SUPPRESSION IN MAMMALS Russian patent published in 1999 - IPC

FIELD: organic chemistry, medicine, oncology, pharmacy. SUBSTANCE: invention relates to compound of the formula (I) where R is C₁-C₁₀-alkyl, phenyl or C₇-C₁₀-aralkyl, C₂-C₁₀-alkyl substituted with one or two substituents taken from a group consisting of OR₁ and NR₂R₃, C₂-C₁₀-alkyl broken by one or two oxygen atoms or a member taken from a group consisting of NR₄, cis-CH= CH-, trans-CH=CH-, -C=C- and optionally substituted with one or two hydroxyls (OH) or NR₂R₃-groups and where R₁ is taken from a group consisting of hydrogen atom, C₁-C₆-alkyl, phenyl, C₇-C₁₀-aralkyl, -CHO, -COR₅,-S(O₂)R₅ and C₂-C₆-alkyl optionally substituted with -NR₂R₃; R₂ and R₃ are similar or distinct and taken from a group consisting of hydrogen atom, C₁-C₁₀-alkyl, C₇-C₁₀-aralkyl, phenyl, C₂-C₁₀-alkyl substituted with one or two hydroxyls (OH), -CHO, -COR₅,COOR₅ and ; R₂ and R₃ taken with nitrogen atom to which they are bound form ethyleneimine ring or 5- or 6-membered aromatic or nonaromatic heterocycle optionally containing another heteroatom taken from a group consisting of sulfur, oxygen and nitrogen atom; R₂ is H and R₃ is -C=(NH)NH₂ or R₂ is -C=(NH)NH₂ and R₃ is H; R₄ is taken from a group consisting of hydrogen atom, C₁-C₁₀-alkyl, C₂-C₁₀-hydroxyalkyl, C₂-C_10/ -alkyl substituted with -NR₂R₃, C₇-C₁₀-aralkyl, α,β or V-naphthyl, phenyl, o-, m- or p-tolyl as a free base or its salt with a pharmaceutically acceptable acid. Compounds show cytostatic and antitumor activity. Invention describes a method of synthesis of compounds of the formula (I) and a method of SUPPRESSION of tumors in mammals by administration of a compound of the formula (I) at the dose from 1 to 50 mg/kg body mass per a day. EFFECT: improved method of synthesis, antitumor activity of compounds synthesized. 38 cl, 12 tbl, 30 ex