Synthesis, biological evaluation and DNA binding properties of novel mono and bisnaphthalimides

A novel series of mono and bisnaphthalimides was synthesized and their antiproliferative activities were evaluated against three tumor cell lines. Bisnaphthalimides 3 and 4, bearing a pyrazine ring fused to the naphthalimide system, showed activities in the order of 10(-8) microM, similar to elinafi...

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Veröffentlicht in:	Organic & biomolecular chemistry 2003-02, Vol.1 (4), p.648-654
Hauptverfasser:	Braña, Miguel F, Cacho, Mónica, Ramos, Ana, Domínguez, M Teresa, Pozuelo, Jose M, Abradelo, Cristina, Rey-Stolle, M Fernanda, Yuste, Mercedes, Carrasco, Carolina, Bailly, Christian
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Cell Division - drug effects Cell Line, Tumor Comet Assay DNA - chemistry DNA Damage Humans Intercalating Agents - chemical synthesis Intercalating Agents - pharmacology Naphthalenes - chemical synthesis Naphthalenes - chemistry Naphthalenes - pharmacology Structure-Activity Relationship Topoisomerase I Inhibitors Topoisomerase II Inhibitors
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Beschreibung
Zusammenfassung:	A novel series of mono and bisnaphthalimides was synthesized and their antiproliferative activities were evaluated against three tumor cell lines. Bisnaphthalimides 3 and 4, bearing a pyrazine ring fused to the naphthalimide system, showed activities in the order of 10(-8) microM, similar to elinafide. DNA binding properties and the ability to induce DNA damage were studied for some of the most active compounds.
ISSN:	1477-0520 1477-0539
DOI:	10.1039/b209042b