SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW ANTHRACYCLINES

Abstract

New anthracyclines including 2-deoxy-L-fucose, 2-deoxy-L-rhamnose and 2, 6-dideoxy-2-iodo-α-L-mannose as sugar moieties, respectively 8, 11 and 14, have been obtained by glycosidation of the 4-demethoxy-9-hydroxymethyl-9-deacetyl daunorubicinone (1) with appropriate sugars under Koenigs-Knorr conditions. They were found to display high cytotoxicity on L1210 leukemia, but also an outstanding antileukemic activity in mice in the case of 8 and 14.