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Meier, Christopher; Steinhauer, Tamara N.; Koczian, Fabian; Plitzko, Birte; Jarolim, Katharina; Girreser, Ulrich; Braig, Simone; Marko, Doris; Vollmar, Angelika M.; Clement, Bernd (2017): A Dual Topoisomerase Inhibitor of Intense Pro-Apoptotic and Antileukemic Nature for Cancer Treatment. In: ChemMedChem, Vol. 12, No. 5: pp. 347-352
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Classic cytotoxic drugs remain indispensable instruments in antitumor therapy due to their effectiveness and a more prevalent insensitivity toward tumor resistance mechanisms. Herein we describe the favorable properties of 6-(N,N-dimethyl-2-aminoethoxy)-11-(3,4,5-trimethoxyphenyl)pyrido[3,4-c][1,9]phenanthroline (P8-D6), a powerful inducer of apoptosis caused by an equipotent inhibition of human topoisomerase I and II activities. A broad-spectrum effect against human tumor cell lines at nanomolar concentrations, as well as strong antileukemic effects, were shown to be superior to those of marketed topoisomerase-targeting drugs and dual topoisomerase inhibitors in clinical trials. The facile four-step synthesis, advantageous drugability properties, and initial invivo data encourage the application of P8-D6 in appropriate animal tumor models and further drug development.