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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Bibliographic Details
Published in:Organic & biomolecular chemistry 2003-02, Vol.1 (4), p.648-654
Main Authors: 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: Article
Language:English
Subjects:
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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Summary: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