SYNTHESIS AND STUDY OF STRUCTURE-ACTIVITY-RELATIONSHIPS OF NEW CLASSES OF ANTHRACYCLINES

Structure-activity studies in the field of anthracyclines have been very fruitful in defining those moieties that are necessary to produce derivatives active on MDR tumor cells. We have found that substitutions on the sugar part of anthracyclines are fundamental to confer activity on MDR cells in vitro. In particular, compounds substituted at C-3' of the sugar moiety with 4-morpholino group or selected potential alkylating moieties are able to overcome resistance both in vitro and in vivo.