11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.

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.

DOI: 10.1016/j.bmc.2008.08.018

Cite this paper

@article{Feng200811Substituted2D, title={11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.}, author={Wei Feng and Mavurapu Satyanarayana and Yuan-Chin Tsai and Angela Aiping Liu and Leroy F. Liu and Edmond J Lavoie}, journal={Bioorganic & medicinal chemistry}, year={2008}, volume={16 18}, pages={8598-606} }