Four new arene–ruthenium(II) complexes [(η6-p-cymene)RuCl(dpm)], where dpm are hexa-(L3–L5) and meso-substituted (L6) dipyrromethene ligands, were synthesized. These ligands and the corresponding complexes were thoroughly characterized by elemental analysis and spectroscopic techniques (MS, IR, 1H, 13C NMR, and UV–vis), and the structures of one ligand and three ruthenium complexes were determined by X-ray single-crystal analysis. The DNA-binding ability of the Ru-3–Ru-6 complexes was evaluated by UV–vis DNA titration. Compound Ru-3 exhibited the highest binding energy, outperforming the complexes containing a dipyrrin ligand substituted by chlorides (Ru-4 and Ru-5) or a meso-substituted dipyrrin (Ru-6). Molecular docking revealed that the hypothetical Ru-1 and Ru-2 complexes, which contain iodide ligands in the dipyrrin structures, showed higher DNA-binding affinities than Ru-3. Computational calculations supported the experimental results, confirming that Ru-3 has a higher affinity for DNA than the other complexes.
About 95 % of candidiasis infections worldwide are attributed to five Candida fungi species, with C. albicans being the most prevalent and severe. Due to resistance phenomena, the last decade has seen a significant challenge for candidiasis treatment with antifungal drugs, which has led to an urgent need for new antifungal agents. In this article, we report the synthesis of a series of azomethine‐pyrazole derivatives bearing a para ‐substituted azo‐phenyl ring. These compounds were evaluated as antifungal agents against Candida species and Cryptococcus neoformans strains. Compound ClAzoNH , substituted by chloride, displayed the highest toxicity on Candida albicans , with an MIC 50 value of 2.08 μg/mL, while methoxy‐substituted MeOAzoNH showed moderate inhibitory activity. The unsubstituted AzoNH compound exhibited the highest activity towards Candida tropicalis , Candida glabrata , Candida parapsilosis , and Candida krusei strains. In the case of C. albicans , the Ca CYP51 protein appears to be the most probable biological target, while for C. neoformans , interactions with the Cn FTase protein explained the in vitro results.
El cáncer es una de las enfermedades que más afecta a la población mundial. Los tratamientos más aplicados son la cirugía, la radioterapia y la quimioterapia. La quimioterapia consiste en el uso de fármacos para destruir las células cancerosas. Sin embargo, puede presentar baja eficiencia, resistencia al tratamiento, y debido a la falta de selectividad del fármaco, provocar efectos secundarios severos. Debido a estas limitaciones, han surgido terapias emergentes, como la terapia fotodinámica (PDT, por sus siglas en inglés). La PDT consiste en administrar al tumor un fotosensibilizador (PS, por sus siglas en inglés), el cual es posteriormente estimulado con una fuente de luz y se producen especies reactivas de oxígeno tóxicas para las células. La PDT ofrece una mayor selectividad hacia las células cancerosas ya que el fotosensibilizador puede inyectarse y activarse de manera localizada y de esta manera no afectar a otros órganos cercanos. Se espera que la PDT en un futuro cercano pudiera ser una terapia valiosa para el tratamiento del cáncer y permitir una mejora en la calidad de vida de los pacientes. DOI: https://doi.org/10.54167/tch.v17i4.1355