Abstract
Several 11-substituted benzo[ i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[ i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC 50 values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.
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