FIELD: chemistry of organophosphate compounds. SUBSTANCE: products: 2-bis-(b -chloroethyl) -amino- (I) or 2-phenoxy -5,7-dimethyl -2,6-dioxo -1,3-diaza -2-phosphaadamantan- es (II). New derivatives of I and II were synthesized. Synthesis of I or II is carried out from 1,5-dimethyl -9-oxo-3,7 -diazabicyclo (3,3,1)nonane and bis-(b -chloroethyl)-amide dichloroanhydride or phosphoric acid phenyl ester in the medium of absolute benzene in the presence of triethylamine at stirring for 2 h followed by evaporation and precipitation of the end I or II with water from the residue. Yield, m. p. C; I 71.4; 145-146; II 52.3; 194-195. I and II show antitumor activity against sarcoma, leukosis and exibit therapeutic effect (% tumor growth inhibition): 33.6-35 for I and 42.0-52.5 for II as compared with that for 25-49 for 5-fluorouracil. Lethal dose LD100 and maximally tolerated dose MTD for I and II 1000 and 850; 2500 and 2000 (200 and 75 for 5-fluorouracil, respectively). Synthesized compounds can be used in medicine. EFFECT: enhanced effectiveness of compounds synthesized. 2 tbl
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Year |
Author |
Number |
| DIHYDROCHLORIDE 1-(3-NITRO-4- METHOXYBENZENE)-2- [BIS-(2- CHLORETHYL) AMINOMETHYL]IMIDAZOLE POSSESSING ANTITUMOR ACTIVITY |
1981 |
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- Garibdzhanjan B.T.
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SU976654A1 |
| 5-BENZIL-11,13-DIMETHHYL-2,8,12-TRIOXO-1,5,9-TRIAZACYCLO [9,3,1,1] HEXADECANE, POSSESSING ANTITUMOR ACTIVITY |
1985 |
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- Chachojan A.A.
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SU1285754A1 |
| 1-(4-AMYLHYDROXY-3-NITROBENZYL)-2-METHYL-4-NITRO-5-[BIS-(2- CHLOROETHYL)-AMINOETHYL]-THIOIMIDAZOLE HYDROCHLORIDE SHOWING ANTITUMOR ACTIVITY |
1985 |
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SU1314627A1 |
| METHOD FOR PRODUCTION OF 2-PHENOXY-5,7-DIMETHYL-2,6-DIOXO-1,3-DIAZA-2-PHOSPHADAMANTHANE |
1988 |
- Agadzhanjan Ts.E.
- Saakjan G.S.
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SU1529695A1 |
| 4(5)-(3-NITRO-4-(3,3-DIMETHYLTRIAZENO-1)PHENYL)IMIDAZOLE POSSESSING ANTITUMOR ACTIVITY |
1982 |
- Iradjan M.A.
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- Arsenjan F.G.
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SU1074091A1 |
| 2,2-DIMETHYL-1,2-DIHYDRO-5-(N-MORPHOLINE)-8-CHLOR OR PHENYLHYDRAZINO-4H-PIRANO[4′,3′:4,5]PYRIDO[2,3-B]THIENO[3,2-D]-9,10,11-TRIAZINES HAVING ANTITUMOR ACTION |
1988 |
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SU1570274A1 |
| N-{4-[BIS-(2- CHLOROETHYL)- AMINO]- PHENYLACETYL} -2-(4-FLUOROPHENYL)-DL-ALANINE HAVING ANTITUMORAL EFFECT |
1988 |
- Kljukene R.B.
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- Shimkjavichene V.J.
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SU1568480A1 |
| 1,3-DIGLYCIDYL-2,4-QUINAZOLINEDIONE SHOWING ANTITUMOR ACTIVITY |
1988 |
- Losev G.A.
- Korotkikh N.I.
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SU1547277A1 |
| 6-[X-(2-HYDROXYETHYL)AMINOALKYL]-5,11-DIOXO-5,6-DIHYDRO- 11H-INDENO [1,2-C]ISOQUINOLINES OR SALTS THEREOF WITH INORGANIC AND ORGANIC ACIDS, METHODS OF PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION BASED THEREON |
1992 |
- Jirzhi Mikhalsky
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- Milan Melka
- Milan Miko
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- Milan Ferents
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- Ruzhena Rajkhlova
- Anna Kargerova
- Jitka Shediva
- Alois Kolonichny
- Jozef Urbanets
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RU2120939C1 |
| 1,4-DIGLYCIDYL-3-ETHYL-1,2,4-TRIAZOLE-5-ONE SHOWING ANTITUMOR ACTIVITY |
1989 |
- Losev G.A.
- Korotkikh N.I.
- Chernov V.A.
- Shvajka O.P.
- Popov S.A.
|
SU1651525A1 |
