Prodrugs of anthracyclines for chemotherapy via enzyme-monoclonal antibody conjugates.
Anticancer Drug Des
; 9(5): 409-23, 1994 Oct.
Article
in En
| MEDLINE
| ID: mdl-7945725
ABSTRACT
New prodrugs of daunorubicin, 1c, 1e and 2c, including a galactopyranosyl residue linked to the N-3' of the daunosaminyl moiety through substituted o- or p-benzyloxycarbonyl groups were synthesized. Their low cytotoxicity and high stability in plasma fulfil the conditions for antibody-directed enzyme prodrug therapy (ADEPT). Enzymatic hydrolysis using alpha-D-galactosidase gives rise to daunorubicin by subsequent self-elimination of the spacers. However, elimination clearly depends on the aromatic substitution pattern, as demonstrated especially by comparison with non-substituted analogues.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Prodrugs
/
Daunorubicin
/
Immunotoxins
/
Enzyme Therapy
Limits:
Animals
/
Humans
Language:
En
Journal:
Anticancer Drug Des
Journal subject:
ANTINEOPLASICOS
/
FARMACOLOGIA
Year:
1994
Type:
Article
Affiliation country:
France