Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 7 de 7
Filtrar
Más filtros











Base de datos
Intervalo de año de publicación
1.
Environ Sci Pollut Res Int ; 28(10): 12232-12244, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-33405142

RESUMEN

At the watershed scale, soil erosion is a cascading system that includes detachment-transport-deposition processes while sediment yield is the net balance of detachment and deposition at the watershed outlet. Due to the temporal-spatial variations of rainfall and landscapes, the relationships between soil erosion and sediment yield are complex and non-linear. Soil erosion processes and sediment yield at the watershed scale have attracted widespread attention; however, few systematic studies have been performed. In this study, a bibliometric analysis and visualization are used to understand the global research status of soil erosion and sediment yield at the watershed scale and provide a reference for researchers to establish future research directions. The USA and China were the most active contributors and had the most publications and active institutions, while Jean Poesen, D.E. Walling, and Xingmin Mu were the top three lead authors in this field. A keyword evolution analysis showed that determining the relationship between soil erosion and the watershed landscape and identifying the sediment source and off-site environmental and ecological effects caused by soil erosion have attracted considerable research attention. Additionally, significant progress has been made in the study of "connectivity," and future research should integrate connectivity and soil erosion models to explain the soil erosion, sediment transport, and deposition processes at the watershed scale.


Asunto(s)
Sedimentos Geológicos , Suelo , Bibliometría , China , Monitoreo del Ambiente , Erosión del Suelo
2.
J Enzyme Inhib Med Chem ; 25(4): 590-5, 2010 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-20235754

RESUMEN

Sixteen novel depsides were synthesized for the first time. Their chemical structures were clearly determined by (1)H NMR, ESI mass spectra, and elemental analyses. All the compounds were assayed for antibacterial activities against three Gram-positive bacterial strains (Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6538, and Streptococcus faecalis ATCC 9790) and three Gram-negative bacterial strains (Escherichia coli ATCC 35218, Pseudomonas aeruginosa ATCC 13525, and Enterobacter cloacae ATCC 13047) by the MTT method. Compound 2-(2-methoxy-2-oxoethyl)phenyl 5-bromonicotinate (5) exhibited significant antibacterial activities against E. coli ATCC 35218 with an MIC of 0.78 microg/mL, which was superior to the positive control kanamycin B. In addition, compound 5 showed potent inhibitory activity against E. coli-induced interleukin-8 production.


Asunto(s)
Antibacterianos/síntesis química , Antiinflamatorios/química , Escherichia coli/inmunología , Interleucina-8/biosíntesis , Antibacterianos/química , Antibacterianos/farmacología , Antiinflamatorios/síntesis química , Antiinflamatorios/farmacología , Depsidos , Escherichia coli/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Espectrometría de Masa por Ionización de Electrospray , Relación Estructura-Actividad
3.
Bioorg Med Chem ; 18(3): 1117-23, 2010 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-20056425

RESUMEN

A series of long-chain derivatives of chrysin (compounds 3-22) were synthesized to evaluate for their antiproliferative activities against the human liver cancer cell line HT-29 and EGFR inhibitory activity. Among the compounds tested, compounds hexadecyl 2-(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy)acetate (10) and N-hexadecyl 2-(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy)acetamide (20) displayed potent EGFR inhibitory activity with IC(50) values of 0.048 microM and 0.035 microM), comparable to the positive control erlotinib. Docking simulation of compounds 10 and 20 was carried out to illustrate the binding mode of the molecular into the EGFR active site, and the result suggested that compound 10 and 20 can bind the EGFR kinase well. Thus, compounds 10 and 20 with potent EGFR inhibitory activity would be potential anticancer agents.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Receptores ErbB/antagonistas & inhibidores , Receptores ErbB/metabolismo , Flavonoides/química , Flavonoides/farmacología , Antineoplásicos/síntesis química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Receptores ErbB/química , Flavonoides/síntesis química , Humanos , Neoplasias Hepáticas/tratamiento farmacológico , Modelos Moleculares , Unión Proteica
4.
Bioorg Med Chem ; 18(1): 314-9, 2010 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-19914835

RESUMEN

Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene)hydrazinyl)thiazol-4(5H)-one (12) displayed the most potent inhibitory activity (IC(50)=0.09 microM for EGFR and IC(50)=0.42 microM for HER-2), comparable to the positive control erlotinib. Docking simulation was performed to position compound 12 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the thiazolidinone derivatives own high antiproliferative activity against MCF-7. Compound 12 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Receptores ErbB/antagonistas & inhibidores , Receptor ErbB-2/antagonistas & inhibidores , Tiazolidinas/química , Tiazolidinas/farmacología , Antineoplásicos/síntesis química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Receptores ErbB/química , Receptores ErbB/metabolismo , Humanos , Modelos Moleculares , Neoplasias/tratamiento farmacológico , Unión Proteica , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Receptor ErbB-2/metabolismo , Relación Estructura-Actividad , Tiazolidinas/síntesis química
5.
Bioorg Med Chem Lett ; 19(23): 6750-4, 2009 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-19836235

RESUMEN

Fatty acid biosynthesis is essential for bacterial survival. Components of this biosynthetic pathway have been identified as attractive targets for the development of new antibacterial agents. FabH, beta-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram positive and negative bacteria. Three series of Schiff bases containing thiazole template were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 11 and 18 were potent inhibitors of E. coli FabH.


Asunto(s)
3-Oxoacil-(Proteína Transportadora de Acil) Sintasa/antagonistas & inhibidores , Antibacterianos/farmacología , Diseño de Fármacos , Inhibidores Enzimáticos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Tiazoles/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Bacterias Gramnegativas/enzimología , Bacterias Grampositivas/enzimología , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Estereoisomerismo , Tiazoles/síntesis química , Tiazoles/química
7.
Acta Crystallogr Sect E Struct Rep Online ; 64(Pt 2): o489, 2008 Jan 23.
Artículo en Inglés | MEDLINE | ID: mdl-21201512

RESUMEN

The title compound, C(18)H(18)FNO(3), consists of three individually planar subunits, namely two substituted benzene rings and one amino-acrylate group. The dihedral angle between the two benzene rings is 47.48 (8)°. The amino-acrylate group forms dihedral angles of 57.95 (7) and 11.27 (6)° with the methoxy-phenyl and fluorophenyl rings, respectively.

SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA