Amonafide- and elinafide-related mono and bisintercalators, modified by the introduction of a pi-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.
Substitution of La(3+) by Sr(2+) in the double perovskite La(2)CoTiO(6) yields materials of the La(2-x)Sr(x)CoTiO(6) series showing a significant amount of trivalent cobalt ions when prepared at ambient atmosphere. The as-prepared compounds can be reduced in severe conditions retaining the perovskite structure while inducing the formation of a large amount of oxygen vacancies. The limit of aliovalent substitution in this series was found to extend up to x = 1. For substitution of La(3+) up to 15% cobalt and titanium are ordered, though the order is progressively lost as x increases; for x≥ 0.30 no ordering is observed as evidenced by magnetic measurements. The ability of these materials to present either cobalt ions in a mixed oxidation state or large amounts of anion vacancies depending on the atmosphere makes them interesting to be further investigated regarding their electrical and electrochemical properties, and hence, their usefulness in some electrochemical devices.
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.
A series of quinoline derivatives as aza analogues of the naphthalene chromophore and a series of "nonfused" tricyclic aromatic systems, in particular 5-arylquinolines and 5- or 6-aryl and heteroaryl naphthalene systems, were synthesized and evaluated for growth-inhibitory properties in several human cell lines. The analysis of quantitative structure-antitumor activity relationships for the growth-inhibitory properties is also reported. Findings suggest that these compounds may not express their cytotoxicity via interaction on DNA.
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