RESUMO
Pazopanib (trade name Votrient®) is a potent and selective multi-targeted tyrosine kinase inhibitor that blocks tumor growth and inhibits angiogenesis. Based on a recently reported procedure, we herein report the first synthesis of four potential process impurities generated in the production of pazopanib. The structure of these impurities were synthesized and characterized by 1H NMR, 13C NMR and HRMS data. The possible formation mechanisms of these impurities were also elucidated. These findings should be useful for the quality control of pazopanib in manufacture.
Assuntos
Inibidores da Angiogênese/química , Contaminação de Medicamentos , Inibidores de Proteínas Quinases/química , Pirimidinas/química , Sulfonamidas/química , Indazóis , Espectroscopia de Ressonância Magnética/métodos , Controle de QualidadeRESUMO
The Asian longhorn beetle (ALB) Anoplophora glabripennis is one of the most successful and most feared invasive insect species worldwide. This review covers recent research concerning the distribution of and damage caused by ALB, as well as major efforts to control and manage ALB in China. The distribution and destruction range of ALB have continued to expand over the past decade worldwide, and the number of interceptions has remained high. Detection and monitoring methods for the early discovery of ALB have diversified, with advances in semiochemical research and using satellite remote sensing in China. Ecological control of ALB in China involves planting mixtures of preferred and resistant tree species, and this practice can prevent outbreaks. In addition, strategies for chemical and biological control of ALB have achieved promising results during the last decade in China, especially the development of insecticides targeting different stages of ALB, and applying Dastarcus helophoroides and Dendrocopos major as biocontrol agents. Finally, we analyze recommendations for ALB prevention and management strategies based on native range and invasive area research. This information will hopefully help some invaded areas where the target is containment of ALB.
Assuntos
Besouros , Inseticidas , Animais , Madeira , ÁrvoresRESUMO
Six novel dibenzyl bromophenols (1-6) with different dimerization patterns and two propyl bromophenol derivatives (7 and 8), together with 11 known bromophenol derivatives, were isolated from the ethanolic extract of the brown alga Leathesia nana. On the basis of spectroscopic methods the structures of the new compounds were determined as 5,6'-diethyloxymethyl-3,4,2'-tribromo-2,3',4'-trihydroxydiphenyl ether (1), 2-(2,3-dibromo-4,5-dihydroxybenzyl)-3,5-dihydroxy-4-methoxybenzyl alcohol (2), 6-(2,3-dibromo-4,5-dihydroxybenzyl)-2,3-dibromo-4,5-dihydroxy benzyl methyl ether (3), 9,10-dihydro-9,10-dimethoxy-3,4,7,8-tetrabromo-1,2,5,6-tetrahydroxyanthracene (4), (+)-3-(2,3-dibromo-4,5-dihydroxyphenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroisobenzofuran (5), rel-(4aS,10aR)-(+/-)-6,7-dibromo-4a-hydroxy-3,8-dihydroxymethyl-10a-methoxy-1,4,4a,10a-tetrahydrodibenzo[b,e][1,4]dioxin-1-one (6), (E)-2-methyl-3-(2,3-dibromo-4,5-dihydroxyphenyl)propenal (7), and 2-methyl-3-(2,3-dibromo-4,5-dihydroxyphenyl)-1-propanol (8). Some compounds including 3 showed in vitro selective cytotoxicity against several human cancer cell lines. This is the first brown alga to be reported containing bromophenols.