Synthesis and evaluation of new antitumor 3-aminomethyl-4,11-dihydroxynaphtho[2,3-f]indole-5,10-diones

A series of new 3-aminomethyl-4,11-dihydroxynaphtho[2,3-f]indole-5,10-diones 6–13 bearing the cyclic diamine in the position 3 of the indole ring was synthesized. The majority of new compounds demonstrated a superior cytotoxicity than doxorubicin against a panel of mammalian tumor cells with determi...

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Veröffentlicht in:	European journal of medicinal chemistry 2014-10, Vol.86, p.797-805
Hauptverfasser:	Shchekotikhin, Andrey E., Glazunova, Valeria A., Dezhenkova, Lyubov G., Luzikov, Yuri N., Buyanov, Vladimir N., Treshalina, Helena M., Lesnaya, Nina A., Romanenko, Vladimir I., Kaluzhny, Dmitry N., Balzarini, Jan, Agama, Keli, Pommier, Yves, Shtil, Alexander A., Preobrazhenskaya, Maria N.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antitumor activity Cattle Cell Proliferation - drug effects Cell Survival - drug effects Circumvention of multidrug resistance DNA - drug effects DNA Cleavage - drug effects DNA ligands DNA Topoisomerases, Type I - metabolism DNA Topoisomerases, Type II - metabolism Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Female Humans Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology K562 Cells Mice Mice, Inbred C57BL Mice, Inbred DBA Molecular Structure Naphtho[2,3-f]indole-5,10-diones Naphthols - chemical synthesis Naphthols - chemistry Naphthols - pharmacology Structure-Activity Relationship Topoisomerase 1/2 inhibitors Topoisomerase Inhibitors - chemical synthesis Topoisomerase Inhibitors - chemistry Topoisomerase Inhibitors - pharmacology Tumor Cells, Cultured
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