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Synthesis and biological evaluation of Chromenylurea and Chromanylurea derivatives as anti-TNF-α agents that target the p38 MAPK pathway.
Li, Xingzhou; Zhou, Xinming; Zhang, Jing; Wang, Lili; Long, Long; Zheng, Zhibing; Li, Song; Zhong, Wu.
Afiliación
  • Li X; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. xingzhou1970@gmail.com.
  • Zhou X; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. chemistry20120720@gmail.com.
  • Zhang J; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. rayzhangjing@sina.com.
  • Wang L; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. Wangll63@126.com.
  • Long L; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. long072811@126.com.
  • Zheng Z; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. zzbcaptain@aliyun.com.
  • Li S; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. lis.lisong@gmail.com.
  • Zhong W; Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China. zhongwu@bmi.ac.cn.
Molecules ; 19(2): 2004-28, 2014 Feb 13.
Article en En | MEDLINE | ID: mdl-24531217
ABSTRACT
A series of 1-aryl-3-(2H-chromen-5-yl)urea and 1-aryl-3-(chroman-5-yl)urea derivatives were designed, synthesized and evaluated for their inhibitory activities towards TNF-α production in lipopolysaccharide-stimulated THP-1 cells. The most active compound, 40g, inhibited TNF-α release with an IC50 value of 0.033 µM, which is equipotent to that of BIRB796 (IC50 = 0.032 µM).
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Urea / Benzopiranos / Factor de Necrosis Tumoral alfa Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2014 Tipo del documento: Article País de afiliación: China
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Urea / Benzopiranos / Factor de Necrosis Tumoral alfa Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2014 Tipo del documento: Article País de afiliación: China