59417-09-3Relevant academic research and scientific papers
New Analogues of Amonafide and Elinafide, Containing Aromatic Heterocycles: Synthesis, Antitumor Activity, Molecular Modeling, and DNA Binding Properties
Bra?a, Miguel F.,Cacho, Mónica,García, Mario A.,De Pascual-Teresa, Beatriz,Ramos, Ana,Domínguez, M. Teresa,Pozuelo, José M.,Abradelo, Cristina,Rey-Stolle, María Fernanda,Yuste, Mercedes,Bá?ez-Coronel, Mónica,Lacal, Juan Carlos
, p. 1391 - 1399 (2007/10/03)
Amonafide- and elinafide-related mono and bisintercalators, modified by the introduction of a π-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, was 2.5-fold more potent than elinafide against human colon carcinoma cells (HT-29). Molecular dynamic simulations and physicochemical experiments have demonstrated that these compounds are capable of forming stable DNA complexes. These results, together with those previously reported by us for imidazo- and pyrazinonaphthalimide analogues, have prompted us to propose that the DNA binding process does not depend on the electronic nature of the fused heterocycle.
