FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention proposes derivatives of acridine of the formula (I): 
where R0 means hydrogen, halogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkylthio, amino-, nitro-group; ρ means 1 or when R0 means C1-C4-alkoxy then ρ means 2 or 3; R1 means hydrogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkylthio; R2 means hydrogen, C1-C4-alkyl; A means oxygen, sulfur, bond, group -(CH2)lNR9, where l means 0 or 1, and R9 means hydrogen or methyl; B means C1-C4-alkylene optionally substituted with hydroxyl group except for that hydroxyl group and part of A can not be bound with the same carbon atom when A means oxygen or sulfur atom, or group (CH2)lR9,, or when A means bond then B means C2-C4-alkylene chain; R3 means hydrogen, C1-C4-alkyl; m = 1 or 2; R4 means hydrogen or halogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkylthio; R5 means hydrogen, C1-C4-alkoxy; R6 means hydrogen, C1-C4/ -alkyl, C1-C4-alkoxy; R7 means hydrogen, or R3 and R7 form together group -(CH2)n- where n = 1 or 2; R8 means hydrogen, C1-C4-alkoxy being group of the formula (a): 
is bound with benzene ring at position 3 or 4 with respect to carboxamide substituent at condition that when group is bound to benzene ring at position 3 then R6 should be at position 6 of benzene ring, or its physiologically acceptable salts. Invention proposes also derivatives of acridine of the formula (Ia): 
where R0 means hydrogen, halogen, C1-C4-alkyl, C1-C4-alkoxy; R1 means hydrogen, C1-C4-alkyl, C1-C4-alkoxy; R2 means hydrogen; A means oxygen, sulfur, bond; B means nonsubstituted C1-C4-alkylene chain; R4 and R5 are similar and mean C1-C4-alkoxy, or their physiologically acceptable salts. Derivatives of acridine of the general formula (I) are synthesized by interaction of compound (II): 
where values 
are given above with compound (III): 
where values A, B, R3-R8 are given above in the presence of coupling reaction agent. Further, physiologically compatible salts of compound (I) can be obtained also. Derivative of acridine of the general formula (I) can be synthesized by interaction of compound of the formula (IV) 
where values R0, R1, R2, R6, A, B, p are given above; Q means halogen atom with compound of the formula (V): 
or its salt where values R3-R5, R7, R8, are given above in the presence of an acid acceptor. Physiologically compatible salts of compound (I) can be obtained also. Invention can be used in medicine to enhance sensitivity of multiple-resistant cancer cells to chemiotherapeutic agents. Method of tumor destruction involves its treatment with compound of the formula (I) or (Ia) or their salts. Pharmaceutical composition has the above indicated compounds. Composition can be made as peroral, buccal, parenteral or rectal forms. EFFECT: improved methods of synthesis, enhanced effectiveness of compounds synthesized. 12 cl, 138 ex
| Title | Year | Author | Number |
|---|---|---|---|
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