| Abstract
| - Amonafide- and elinafide-related mono and bisintercalators, modified by the introduction of aπ-excedent furan or thiophene ring fused to the naphthalimide moiety, have been synthesized.These compounds have shown an interesting antitumor profile. The best compound, 9, was2.5-fold more potent than elinafide against human colon carcinoma cells (HT-29). Moleculardynamic simulations and physicochemical experiments have demonstrated that these compounds are capable of forming stable DNA complexes. These results, together with thosepreviously reported by us for imidazo- and pyrazinonaphthalimide analogues, have promptedus to propose that the DNA binding process does not depend on the electronic nature of thefused heterocycle.
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