Structure-activity relationships for acridine-substituted analogues of the mixed topoisomerase I/II inhibitor N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.

@article{Spicer1997StructureactivityRF,
  title={Structure-activity relationships for acridine-substituted analogues of the mixed topoisomerase I/II inhibitor N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.},
  author={Julie A. Spicer and Swarna A. Gamage and Graham J. Atwell and Graeme Finlay and B. C. Baguley and William A. Denny},
  journal={Journal of medicinal chemistry},
  year={1997},
  volume={40 12},
  pages={1919-29}
}
The mixed topoisomerase I/II inhibitor N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) is currently in clinical trial as an anticancer drug. A series of acridine-substituted analogues were prepared, using a new synthetic route to substituted acridine-4-carboxylic acids (conversion of substituted diphenylamine diacid monoesters to the corresponding aldehydes and mild acid-catalyzed ring closure to form the acridines directly). The analogues were evaluated in a panel of cell lines which… CONTINUE READING

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