SYNTHESIS OF NEW MALEIMIDE DERIVATIVES OF DAUNORUBICIN AND BIOLOGICAL-ACTIVITY OF ACID-LABILE TRANSFERRIN CONJUGATES

Authors
KRATZ F BEYER U SCHUMACHER P KRUGER M ZAHN H ROTH T FIEBIG HH UNGER C
Citation
F. Kratz et al., SYNTHESIS OF NEW MALEIMIDE DERIVATIVES OF DAUNORUBICIN AND BIOLOGICAL-ACTIVITY OF ACID-LABILE TRANSFERRIN CONJUGATES, Bioorganic & medicinal chemistry letters, 7(5), 1997, pp. 617-622
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
5
Year of publication
1997
Pages
617 - 622
Database
ISI
SICI code
0960-894X(1997)7:5<617:SONMDO>2.0.ZU;2-Z
Abstract
Maleimide groups were bound to the 3'-amino position of daunorubicin t hrough a benzamide bond or to the 13-keto position through a benzoyl h ydrazone or phenylacetyl hydrazone bond. The acid labile transferrin c onjugates prepared with the latter two derivatives exhibited high acti vity in human melanoma cells (MEXF 989) using a clonogenic cell assay comparable to or exceeding that of daunorubicin. (C) 1997 Elsevier Sci ence Ltd. All rights reserved.