Bioorganic and Medicinal Chemistry Letters p. 617 - 622 (1997)
Update date:2022-08-17
Topics:
Kratz, Felix
Beyer, Ulrich
Schumacher, Peter
Krueger, Michael
Zahn, Heike
Roth, Thomas
Fiebig, Heinz H.
Unger, Clemens
Maleimide groups were bound to the 3'-amino position of daunorubicin through a benzamide bond or to the 13-keto position through a benzoyl hydrazone or phenylacetyl hydrazone bond. The acid labile transferrin conjugates prepared with the latter two derivatives exhibited high activity in human melanoma cells (MEXF 989) using a clonogenic cell assay comparable to or exceeding that of daunorubicin.
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