6((2-HYDROXYETHYL)AMINOALKYL)-5,11-DIOXO-5,6-DIHYDRO-11-H- INDENO-(1,2-C)ISOQUINOLINE AND THEIR USE AS ANTINEOPLASTIC AGENTS

New 6-[X-(2-hydroxyethyl)aminoalkyl]-5,11-dioxo-5,6-dihydro-11H-indeno[1,2 -c]isochinoline derivatives represented by general formula (I), in which X stands for the number of carbon atoms from 0 to 5 in aminoalkyl group situated on nitrogen atom in position 6 of the indenoisochinoline fundamental st...

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Hauptverfasser: MILAN FERENC, JIRI HRBATA, IRENA KEJHOVA, ALOIS KOLONICNY, JIRI KREPELKA, RZENA REICHLOVA, ANNA KARGEROVA, JOSEF URBANEC, EVA SKACELOVA, MILAN MIKO, MILAN HRUBY, MILAN MELKA, JITKA SEDIVA
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creator MILAN FERENC
JIRI HRBATA
IRENA KEJHOVA
ALOIS KOLONICNY
JIRI KREPELKA
RZENA REICHLOVA
ANNA KARGEROVA
JOSEF URBANEC
EVA SKACELOVA
MILAN MIKO
MILAN HRUBY
MILAN MELKA
JITKA SEDIVA
description New 6-[X-(2-hydroxyethyl)aminoalkyl]-5,11-dioxo-5,6-dihydro-11H-indeno[1,2 -c]isochinoline derivatives represented by general formula (I), in which X stands for the number of carbon atoms from 0 to 5 in aminoalkyl group situated on nitrogen atom in position 6 of the indenoisochinoline fundamental structure, their salts with inorganic and organic acids and their derivatives were described. Antitumorously effective indenoisochinoline derivatives are most preferably prepared by the process in which the indeno[1,2-c]isocoumarine and/or 1-methoxy-2-(2-methoxycarbonylphenyl)-1-inden-3-one, respectively, comprises reacting with N-(hydroxyethyl)alkylen diamine in a medium of suitable aprotic solvent, preferably dimethylformamide, and at increased temperature. Another process for the preparation comprises reacting 6-(X-chloroalkyl)-5,11-dioxo-5,6-dihydro-11H-indeno[1,2-c]isochinolines with 2-aminoethanol in suitable solvent, preferably dimethylformamide, in the presence of anhydrous potassium carbonate. New compounds, their derivatives and salts are useful for the preparation of drugs and compositions for the treatment of malignant neoplasias in mammals.
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Antitumorously effective indenoisochinoline derivatives are most preferably prepared by the process in which the indeno[1,2-c]isocoumarine and/or 1-methoxy-2-(2-methoxycarbonylphenyl)-1-inden-3-one, respectively, comprises reacting with N-(hydroxyethyl)alkylen diamine in a medium of suitable aprotic solvent, preferably dimethylformamide, and at increased temperature. Another process for the preparation comprises reacting 6-(X-chloroalkyl)-5,11-dioxo-5,6-dihydro-11H-indeno[1,2-c]isochinolines with 2-aminoethanol in suitable solvent, preferably dimethylformamide, in the presence of anhydrous potassium carbonate. 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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 6((2-HYDROXYETHYL)AMINOALKYL)-5,11-DIOXO-5,6-DIHYDRO-11-H- INDENO-(1,2-C)ISOQUINOLINE AND THEIR USE AS ANTINEOPLASTIC AGENTS
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