N-benzyladriamycin

AD288 (N-benzyladriamycin) is a highly lipophilic, semi-synthetic anthracycline derivative of doxorubicin (Adriamycin). Unlike doxorubicin, which acts as a topoisomerase II poison by stabilizing DNA-cleavable complexes and causing double-stranded DNA breaks, AD288 acts as a catalytic inhibitor of DNA topoisomerase II. It prevents the initial non-covalent binding of topoisomerase II to DNA, primarily through DNA intercalation, thereby blocking enzyme access to DNA binding sites without generating double-strand breaks. AD288 is also the principal active metabolite of the lipophilic anthracycline prodrug AD198 (N-benzyladriamycin-14-valerate). It has been investigated for its antitumor activity, particularly in multidrug-resistant (MDR) cancer models, as it remains active in cells with reduced topoisomerase II activity or P-glycoprotein overexpression.

Other names

N-benzyl doxorubicin