Sabarubicin (MEN 10755) is the progenitor of a third generation of synthetic anthracycline oligosaccharides. Sabarubicin deamino analogues MEN 10959 and MEN 12297 were evaluated for topoisomerase II poisoning, cytotoxic potency and antitumor activity in human xenografts. The new analogues were able to induce DNA cleavage mediated by both DNA topoisomerase IIα and β and a good correlation was found regarding their cytotoxic activity. The two analogues possess also a different spectrum of antitumor activity, compared to sabarubicin.
Keywords: sabarubicin, men 10755, men 10959, men 12297, anthracycline disaccharides, dna topoisomerase
open access plus
Rights & PermissionsPrintExport