Title : Synthesis and biological evaluation of novel prodrugs of anthracyclines for selective activation by the tumor-associated protease plasmin.

Pub. Date : 1999 Dec 16

PMID : 10602713






3 Functional Relationships(s)
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1 New prodrugs of daunorubicin and doxorubicin designed for selective activation by the serine protease plasmin are described. Doxorubicin plasminogen Homo sapiens
2 A marked in vitro selectivity was demonstrated by incubation of the doxorubicin prodrugs with a plasmin generating MCF-7 breast cancer cell line transfected with urokinase-type plasminogen activator (u-PA) in comparison with the nontransfected nonplasmin generating cell line. Doxorubicin plasminogen Homo sapiens
3 Prodrugs 4 and 5 showed the same cytotoxic effect as the free parent drug doxorubicin in the u-PA transfected cells, indicating complete conversion of the prodrug by plasmin. Doxorubicin plasminogen Homo sapiens