NEW 7-ARYL ANALOGS OF ANTHRACYCLINES - SYNTHESIS AND CYTOTOXIC ACTIVITY OF (+ )-7-(3,4,5-TRIMETHOXYPHENYL)-7-DEOXYIDARUBICINONE/

The synthetic methodology for the preparation of 7-aryl-7-deoxyanthrac yclinones, a new class of anthracycline analogues, is described. Readi ly available materials are easily transformed into the key intermediat e ketone, that is converted into bent and planar tetracyclic compounds . Cytotoxic studies of the final and intermediate products reveal a mo derate activity of bent products and a lack of activity of planar prod ucts, thus supporting a non-intercalating mechanism for their cytotoxi c activity. (C) 1997 Elsevier Science Ltd.