FIELD: biochemistry, nucleosides. SUBSTANCE: product of the general formula where R - R-BrCH2 (I) or R - 
(II) as specific irreversible inhibitors of RNA-polymerase. Synthesis is carried out by selective acylation of guanosine hydrochloride in anhydrous phosphoric acid hexamethyltriamide with chloroanhydride of corresponding 4-substituted benzoic acid. Value K for compounds (I) and (II) - 0.13 and 0.09 min-1, respectively, and for analog - guanosine-5′-(2-bromoethyl)-phosphonate lithium salt value Kg = 0.03 min-1. Use of compound (II) ensures to identify SH-group in active site of enzyme also. EFFECT: improved method of synthesis, increased effectiveness of synthesized compounds as RNA-polymerase inhibitors.
| Title |
Year |
Author |
Number |
| HALOID-CONTAINING 3'-AMIDODERIVATIVES OF (1'R,5'R)-3' -AZA-1'-(2-AMINO -1,6-DIHYDRO -6-OXOPURINYL-9) -3'-DEOXYPYRANOSIDE AS SPECIFIC IRREVERSIBLE FLUORESCENT INHIBITORS OF RNA-POLYMERASE |
1991 |
- Khropov Ju.V.
- Baranova L.A.
- Tunitskaja V.L.
- Kochetkov S.N.
|
RU2039065C1 |
| 4-AZIDONAPHTHALENE-1-SULFONYLCHLORIDE AS SEMIPRODUCT FOR SYNTHESIS OF (1′R,5′R) -3′-AZA-1′ -(2-AMINO-1,6-DIHYDRO-6-OXOPURINYL-9)-- 3′-DEOXY-3′- (4-AZIDONAPHTHALENE-1-SULFAMIDO) HEXOPYRANOSYL-- 6′-TRIPHOSPHATE TRILITHIUM SALT AS SPECIFIC PHOTOACTIVATED IRREVERSIBLE RNA-POLYMERASE INHIBITOR |
1991 |
- Kulagin S.V.
- Seliverstov V.O.
- Khropov Ju.V.
- Mishin A.A.
- Kochetkov S.N.
|
RU2036902C1 |
| (1′R,5′R)-3′-AZA-1′- (2-AMINO-1,6-DIHYDRO-6- OXOPURINYL-9)-3′-DEOXY- 3′- (AZIDONAPHTHALENE-1-SULFAMIDO) -HEXOPYRANOSYL-6′-TRIPHOSPHA- TE TRILITHIUM SALTS AS SPECIFIC PHOTOACTIVATED IRREVERSIBLE RNA-POLYMERASE INHIBITORS |
1991 |
- Khropov Ju.V.
- Mishin A.A.
- Seliverstov V.O.
- Kulagin S.V.
- Kochetkov S.N.
|
RU2036928C1 |
| AZIDONAPHTHALENE -1-SULFONYLHYDRAZINES AS SEMIPRODUCTS FOR SYNTHESIS OF (1′R,5′R)-3′-AZA-1′- (2-AMINO-1,6-DIHYDRO-6-OXOPURINYL-9)-- 3′-DEOXY- 3′-(AZIDONAPHTHALENE-1-SULFAMIDO)-HEXOPYRANOSY- L-6′- TRIPHOSPHATES TRILITHIUM SALTS AS SPECIFIC PHOTOACTIVATED IRREVERSIBLE RNA-POLYMERASE INHIBITORS |
1991 |
- Khropov Ju.V.
- Mishin A.A.
- Seliverstov V.O.
- Kulagin S.V.
- Kochetkov S.N.
|
RU2036903C1 |
| 5-FLUOROSULFONYL-BENZOYL DERIVATIVES OF URIDINE FOR SPECIFIC NON-REVERSIBLE INHIBITION OF GLYCOGENE SYNTHESASE |
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- Khropov Yurij Valentinovich
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|
SU1122671A1 |
| METHOD FOR SYNTHESIS OF SUBSTITUTED 5Ъ-(2-HYDROXYBENZOYL)-DERIVATIVES OF PURINE NUCLEOSIDES |
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|
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|
SU1028675A1 |
| LITHIUM SALTS OF (I'R,5'R)-3'-AZA-3'-(AZIDONAPHTHALINE-1- SULFAMIDO)-1'-(6-AMINOPURINYL-9)-3'-DEOXYHEXOPIRANOZYL- 6'-DI-OR TRIPHOSPHATES AS SPESIFIC PHOTOACTIVATED IRREVERSIBLE INHIBITORS OF Na, K-ADENOSINE TRIPHOSPHATASE |
1997 |
- Khropov Ju.V.
- Mishin A.A.
- Seliverstov V.O.
- Kulagin S.V.
- Lopina O.D.
|
RU2130943C1 |
| SALTS OF (1'R, 5'R)-3'-AZA-1'(6-AMINOPURINYL-9)-3'- DEOXYHEXOPYRANOSYL-6'-DIPHOSPHATE 3'-AMIDODERIVATIVES AS SPECIFIC FLUORESCENT INHIBITORS OF MYOSINIC ADENOSINE-5'- TRIPHOSPHATASE |
1997 |
- Baranova L.A.
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|
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| METHODS AND MEANS OF INCREASING PRODUCTIVITY OF RNA |
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|
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