A variety of aminoisoquinoline-5,8-quinones bearing α-amino acids moieties were synthesized from 3-methyl-4-methoxycarbonylisoquinoline-5,8-quinone and diverse L-and D-α-amino acid methyl esters. The members of the series were evaluated for their cytotoxic activity against normal and cancer cell lines by using the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay. From the current investigation, structure-activity relationships demonstrate that the location and structure of the amino acid fragment plays a significant role in the cytotoxic effects. Moderate to high cytotoxic activity was observed and four members, derived from L-alanine, L-leucine, L-phenylalanine, and D-phenylalanine, were selected as promising compounds by their IC 50 ranging from 0.5 to 6.25 µM and also by their good selectivity indexes (≥2.24).
Oximes are known for their anti-inflammatory, antimicrobial, antioxidant, and anticancer activities. Frequently, modification of biologically active carbonyl compounds into oximes leads to increased activity. The present study reports the reactivity of 2-alkanoylnaphthohydroquinones against hydroxylamine under aerial conditions. Results show that, depending on the structure of the hydroquinones, the reaction proceeds through two different chemical pathways to produce 2-(hydroxyamino)-1,4-naphthoquinone and their C-3 (hydroxyimino)alkyl derivatives. Both the formation of the quinoid compounds under aerial oxidation and C-C cleavage reactions of hemiaminal intermediates are discussed. In vitro screening of the substituted 1,4-naphthoquinones on a panel of cancer cells reveals moderate cytotoxic activities. Compound 19, 2-(hydroxyamino)-1,4-naphthoquinone, stands out by its anticancer potency against prostate cancer cells as shown by the lowest IC50 value (8.08 μM) and the best selectivity index (3.90).
Las comunidades costeras de pesca artesanal (conocidas a pequeña escala como "caletas") son sistemas socioecológicos complejos que se adaptan a las perturbaciones dependiendo de su complejidad y propiedades inherentes. La capacidad de evaluar y monitorear esta respuesta adaptativa proporciona información sobre la sostenibilidad de las caletas, necesaria para una planificación estratégica y territorial. Seis caletas ubicadas en el archipiélago de Chiloé, sur de Chile, sirvieron de modelo para identificar la complejidad territorial. En este artículo se identificaron 4 criterios y 16 subcriterios (utilizando el software Expert Choice) como descriptores adecuados de su complejidad y se clasificaron jerárquicamente según su importancia (%). Todas estas variables se fusionaron en un Índice de Complejidad Territorial (ICT), un estimador cualicuantitativo de la sostenibilidad de las caletas. Un Análisis de Componentes Principales incluyó todos los subcriterios y caracterizó la complejidad de las caletas. Este artículo demuestra que la complejidad requiere un análisis integrado de las variables relevantes para el monitoreo de las trayectorias evolutivas de las caletas, ante lo cual, el ICT destaca como una herramienta cuantitativa conveniente para la planificación estratégica y territorial.
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