title: Prodrugs of anthracycline antibiotics suited for tumor-specific activation.
abstract: The two novel prodrugs 4 and 11 have been prepared from tetra-O-acetyl-D-galactopyranose and doxorubicin in three and six steps, respectively. Their low cytotoxicity, high stability in plasma and, in the case of 11, efficient hydrolysis in the presence of alpha-galactosidase, fulfill preliminary conditions for their use in combination with monoclonal antibody-enzyme conjugates.
authors.affiliation: Institut Curie, Section Biologie, Paris, France.
authors.forename: M
authors.initials: M
authors.lastname: Azoulay
authors.forename: J C
authors.initials: JC
authors.lastname: Florent
authors.forename: C
authors.initials: C
authors.lastname: Monneret
authors.forename: J P
authors.initials: JP
authors.lastname: Gesson
authors.forename: J C
authors.initials: JC
authors.lastname: Jacquesy
authors.forename: F
authors.initials: F
authors.lastname: Tillequin
authors.forename: M
authors.initials: M
authors.lastname: Koch
authors.forename: K
authors.initials: K
authors.lastname: Bosslet
authors.forename: J
authors.initials: J
authors.lastname: Czech
authors.forename: D
authors.initials: D
authors.lastname: Hoffman
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000633:toxicity; D004317:Doxorubicin / Q000737:chemistry*; D005697:Galactosides / Q000737:chemistry; D007939:Leukemia L1210; D011355:Prodrugs / Q000737:chemistry* / Q000633:toxicity; D014407:Tumor Cells, Cultured; D000519:alpha-Galactosidase / Q000378:metabolism
chemical_list: D000903:Antibiotics, Antineoplastic; D005697:Galactosides; D011355:Prodrugs; D004317:Doxorubicin; D000519:alpha-Galactosidase