Synthesis of new maleimide derivatives of daunorubicin and biological activity of acid labile transferrin conjugates

✍ Scribed by Felix Kratz; Ulrich Beyer; Peter Schumacher; Michael Krüger; Heike Zahn; Thomas Roth; Heinz H. Fiebig; Clemens Unger

• Book ID: 104364882
• Publisher: Elsevier Science
• Year: 1997
• Tongue: English
• Weight: 385 KB
• Volume: 7
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(97)00069-3

✦ Synopsis

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.