RESUMEN
A magnetically retrievable ferrocene appended supported ionic liquid phase (SILP) photocatalyst containing a molybdate anion has been synthesized and characterized by Fourier transform infrared, X-ray photoelectron spectroscopy, transmission electron microscopy, X-ray diffraction, energy dispersive spectroscopy, and vibrating sample magnetometer analysis. The optical properties of the photocatalyst were probed by photoluminescence and UV-vis diffuse reflectance spectroscopy. The discharge of undesirable dye effluents from textile industrial plants in the environment is the major concern of environmental pollution and toxicity. In this context, we employed the as-prepared SILP photocatalyst for degradation of methyl orange (MO) under UV light (365 nm) irradiation, and subsequently, recycling studies were performed. The histological alteration in gills of the fish is employed as a tool for monitoring toxins in the environment. In view of this, the histo-toxicological assessment on freshwater fish Tilapia mossambica gills asserted the damage of secondary gill lamellae due to MO. Conversely, structural modifications in the gill architecture were not observed by virtue of photodegraded products confirming that the degraded product is nontoxic in nature. Additionally, the normal behavior of fishes on exposure to photodegraded products reveals that research findings are beneficial for the aquatic ecosystem.
RESUMEN
We have recently explored novel class of potentially anti-breast cancer active enamidines in which four molecules 4a-c and 4h showed higher anticancer activity compared to standard drug doxorubicin. As a part of extension of this work, we have further evaluated in silico cheminformatic studies on bioactivity prediction of synthesized series of enamidines using mole information. The normal cell line study of four lead compounds 4a-c and 4h against African green monkey kidney vero strain further revealed that the compounds complemented good selectivity in inhibition of cancer cells. The in silico bioactivity and molecular docking studies also revealed that the compounds have significant interactions with the drug targets. The results reveal that enamidine moieties are vital for anti-breast cancer activity as they possess excellent drug-like characteristics, being potentially good inhibitors of cyclin dependent kinases7 (CDK7).
Asunto(s)
Aminas/farmacología , Antineoplásicos/farmacología , Azidas/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Simulación por Computador , Quinasas Ciclina-Dependientes/antagonistas & inhibidores , Pargilina/análogos & derivados , Inhibidores de Proteínas Quinasas/farmacología , Aminas/síntesis química , Aminas/química , Animales , Antineoplásicos/síntesis química , Antineoplásicos/química , Azidas/síntesis química , Azidas/química , Sitios de Unión/efectos de los fármacos , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/patología , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Chlorocebus aethiops , Quinasas Ciclina-Dependientes/química , Quinasas Ciclina-Dependientes/metabolismo , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Humanos , Enlace de Hidrógeno , Células MCF-7 , Simulación del Acoplamiento Molecular , Estructura Molecular , Pargilina/síntesis química , Pargilina/química , Pargilina/farmacología , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/química , Células Vero , Quinasa Activadora de Quinasas Ciclina-DependientesRESUMEN
In the title mol-ecule, C20H19NO2, the naphthalene ring system subtends a dihedral angle of 82.50â (7)° with the benzene ring and an intra-molecular N-Hâ¯O hydrogen bond closes an S(6) ring. In the crystal, mol-ecules are linked by O-Hâ¯O hydrogen bonds, which generate C(8) chains propagating in the [010] direction. The crystal structure also features weak π-π inter-actions [centroid-centroid separation = 3.7246â (10)â Å].
RESUMEN
A library of quinazolinones was prepared by the one-pot three-component reaction of isatoic anhydride, ammonium salts/amines, and various electrophiles using aqueous hydrotropic solution as an efficient, economical, reusable, and green medium giving good to excellent yields of products in very short time. The method offers a versatile way for the development of diversity-oriented synthesis of quinazolinones.
Asunto(s)
Quinazolinonas/química , Quinazolinonas/síntesis química , Agua/química , Aminas/química , Compuestos de Amonio/química , Catálisis , Técnicas de Química Sintética , Tecnología Química Verde , Oxazinas/químicaRESUMEN
A novel series of ferrocene tagged multi-functionalized 1,4-dihydropyrimidines is synthesized by base catalyzed cyclocondensation between ferrocenyl chalcones and amidines. The structures of synthesized compounds were established on the basis of (1)H NMR, (13)C NMR, FTIR spectroscopy as well as by mass spectrometry. The compounds were evaluated for in vitro anticancer activity. The most active compounds from the series displayed GI50 value equal to doxorubicin against the strain of human breast cancer cell line MDA-MB-435.
Asunto(s)
Antineoplásicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Compuestos Ferrosos/química , Pirimidinas/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Neoplasias de la Mama/patología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Humanos , Metalocenos , Estructura Molecular , Pirimidinas/síntesis química , Pirimidinas/química , Relación Estructura-ActividadRESUMEN
Ultrasound promoted synthesis of ß-amino carbonyl compounds in aqueous hydrotropic medium at ambient temperature is reported. The remarkable features of the new procedure are shorter reaction time, excellent yields in aqueous medium, cleaner reaction profile and simple experimental and work-up procedure.
Asunto(s)
Cetonas/síntesis química , Sonicación , Aldehídos/química , Compuestos de Anilina/química , Interacciones Hidrofóbicas e Hidrofílicas , Cetonas/química , Estructura Molecular , Agua/químicaRESUMEN
The catalytic efficiency in organic synthesis of the aqueous extract of the pericarp of Sapindus trifoliatus fruits was evaluated. The synthesis of a series of aldimines from aromatic aldehydes and amines was successfully catalyzed by the extract, whereas aromatic ketones and amines did not yield ketimines under comparable reaction conditions, indicating the chemoselective catalysis of the extract. The catalytic activity of the extract is due to saponins, which have a common structural skeleton containing a pentacyclic triterpenoid part substituted with different carbohydrate side chains. The mild conditions, high yields, and short reaction times not only make this protocol a valuable alternative to the conventional methods, but it also becomes significant under the roof of environmentally greener and safer processes.