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Prodrugs of the Cytostatic CC‐1065 That Can Be Activated in a Tumor‐Selective Manner

1996; Wiley; Volume: 35; Issue: 22 Linguagem: Inglês

10.1002/anie.199626741

1521-3773

Lutz F. Tietze, Robert E. Hannemann, Wilm Buhr, Michael Lögers, Pia Menningen, Monika Lieb, Dorothea Starck, Thomas Grote, Angela Döring, Ingrid Schuberth,

Monoclonal and Polyclonal Antibodies Research

The O-glycosides 1 of the seco-CI derivative 2, which is the seco form of the simplified pharmacophoric group of the potent cytotoxic antibiotic CC-1065, show only very low toxicity. In tumor-selective cancer therapy they can be used in conjunction with conjugates of glycohydrolases and monoclonal antibodies that bind at tumor-associated antigens. The glycohydrolases cleave the prodrugs 1 and release the cytotoxic components 2.