SYNTHESIS OF NOVEL TARGETED PRO-PRODRUGS OF ANTHRACYCLINES POTENTIALLY ACTIVATED BY A MONOCLONAL-ANTIBODY GALACTOSIDASE CONJUGATE .1.

被引：29

作者：

ANDRIANOMENJANAHARY, S

DONG, X

FLORENT, JC

GAUDEL, G

GESSON, JP

JACQUESY, JC

KOCH, M

MICHEL, S

MONDON, M

MONNERET, C

PETIT, P

RENOUX, B

TILLEQUIN, F

机构：

[1] INST CURIE,CHIM LAB,BIOL SECT,26 RUE ULM,F-75005 PARIS,FRANCE

[2] UNIV PARIS 05,FAC SCI PHARMACEUT & BIOL,PHARMACOGNOSIE LAB,F-75270 PARIS 06,FRANCE

[3] FAC SCI POITIERS,CHIMIE LAB 12,F-86022 POITIERS,FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)80625-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Daunorubicin substituted at N-3' with a benzyloxycarbonyl group (self-immolative spacer) linked to an alpha-D-galactosyl residue such as 7a and 7b have been prepared as prodrugs. Conversion of 7a and 7b to daunorubicin will be mediated by an immunoconjugate consisting of an alpha-D-galactosidase enzyme covalently attached to a tumor specific monoclonal antibody.

引用

页码：1093 / 1096

页数：4

共 23 条

[1] (ACYLOXY)ALKYL CARBAMATE PRODRUGS OF NORFLOXACIN
ALEXANDER, J
FROMTLING, RA
BLAND, JA
PELAK, BA
GILFILLAN, EC
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (01) : 78 - 81
[2] (ACYLOXY)ALKYL CARBAMATES AS NOVEL BIOREVERSIBLE PRODRUGS FOR AMINES - INCREASED PERMEATION THROUGH BIOLOGICAL-MEMBRANES
ALEXANDER, J
CARGILL, R
MICHELSON, SR
SCHWAM, H
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1988, 31 (02) : 318 - 322
[3] Arcamone F., 1981, DOXORUBICIN ANTICANC
[4] THE 1ST BAGSHAWE LECTURE - TOWARDS GENERATING CYTO-TOXIC AGENTS AT CANCER SITES
BAGSHAWE, KD
[J]. BRITISH JOURNAL OF CANCER, 1989, 60 (03) : 275 - 281
[5] BRISTOW MR, 1978, CANCER TREAT REP, V62, P783
[6] A NOVEL CONNECTOR LINKAGE APPLICABLE IN PRODRUG DESIGN
CARL, PL
CHAKRAVARTY, PK
KATZENELLENBOGEN, JA
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1981, 24 (05) : 479 - 480
[7] Conchie J, 1963, METHODS CARBOHYDR CH, V2, P345
[8] DEAN KJ, 1979, J BIOL CHEM, V254, P6
[9] DEY PM, 1967, CHEM IND-LONDON, V39, P1637
[10] SILVER-ASSISTED REACTIONS OF ORGANOTIN OXIDES - A MILD, NEUTRAL AND ANHYDROUS ONE-STEP CONVERSION OF PRIMARY ORGANIC HALIDES TO ALCOHOLS
GINGRAS, M
CHAN, TH
[J]. TETRAHEDRON LETTERS, 1989, 30 (03) : 279 - 282

← 1 2 3 →