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Carboxylated, heteroaryl-substituted chalcones as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases

…, KJ Worsencroft, Z Ye, MD Weingarten…

文献索引:Meng, Charles Q.; Ni, Liming; Worsencroft, Kimberly J.; Ye, Zhihong; Weingarten, M. David; Simpson, Jacob E.; Skudlarek, Jason W.; Marino, Elaine M.; Suen, Ki-Ling; Kunsch, Charles; Souder, Amy; Howard, Randy B.; Sundell, Cynthia L.; Wasserman, Martin A.; Sikorski, James A. Journal of Medicinal Chemistry, 2007 , vol. 50, # 6 p. 1304 - 1315

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被引用次数: 47

摘要

Starting from a simple chalcone template, structure-activity relationship (SAR) studies led to a series of carboxylated, heteroaryl-substituted chalcone derivatives as novel, potent inhibitors of vascular cell adhesion molecule-1 (VCAM-1) expression. Correlations between lipophilicity determined by calculated logP values and inhibitory efficacy were observed among structurally similar compounds of the series. Various substituents were found to be ...