Adriamycin antitumour action

Adriamycin toxicity in CBA mice bearing TLX5 lymphoma was reduced by a pharmacological dose of melatonin (20-40 mg/kg) without decreasing the antitumour action of adriamycin (Rapozzi et al. 1998). 

A considerable amount of research has gone into elucidating the molecular mechanism of action of these antitumour quinones. While several mechanisms are possible, a single mechanism may not fully explain all of the observed cytotoxic effects. One of the objectives of the NCI and other studies elsewhere has been to determine if there were any structure-activity relationships within the major structural groups ranging from the simplest benzoquinones to the complex multiple heteroatom quinones. One of the main conclusions from these studies was that the most active compounds were mitomycin C, the 3,6-diaziridinylbenzoquinones with 2,5-alkylamino substituents, adriamycin (doxorubicin), daunomycin (daunorubicin) and AZQ (Figure 1). 

Adriamycin probably has the widest spectrum of activity of any current antitumour drug but its cardiotoxicity limits the total cumulative dose which can be administered the analogues of adriamycin and daunomycin clinically evaluated to date (for example rubidazone and duborimycin) show no clear advantage over adriamycin. Considerable progress has been made in the study of the actions of... 

---