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Synthesis, Antitumor Activity, Molecular Modeling, and DNA Binding Properties of a New Series of Imidazonaphthalimides

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journal contribution
posted on 22.11.2002, 00:00 by Miguel F. Braña, Mónica Cacho, Mario A. García, Beatriz de Pascual-Teresa, Ana Ramos, Nuria Acero, Francisco Llinares, Dolores Muñoz-Mingarro, Cristina Abradelo, María Fernanda Rey-Stolle, Mercedes Yuste
A series of mono and bisintercalators based on the 5,8-dihydrobenz[de]imidazo[4,5-g]isoquinoline-4,6-dione system were synthesized and evaluated for growth inhibitory properties in several human cell lines. All target compounds showed activity in the micromolar range. Representative compounds were evaluated using UV−vis spectroscopy and viscosimetric determinations, showing that they behave as DNA intercalators. Molecular modeling techniques were used in order to rationalize the moderate activity observed for bisnaphthalimides.