萘取代查尔酮组合文库的合成与筛选：白三烯B4抑制剂
Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: inhibitors of leukotriene B4.
作者信息
Deshpande A M, Argade N P, Natu A A, Eckman J
机构信息
Division of Organic Chemistry (Synthesis), National Chemical Laboratory, Pune, India.
出版信息
Bioorg Med Chem. 1999 Jun;7(6):1237-40. doi: 10.1016/s0968-0896(99)00047-4.
Abstract
A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene B4 inhibitory activity using human whole blood assay (HWBL) afforded a lead compound, 1-(6-butoxy-2-naphthyl)-3-(4-nitrophenyl)-prop-2-en-1-one (K4A3) with an IC50 value of 18.5 microM.
摘要
通过溶液相化学方法制备了一个萘取代查尔酮的组合微型文库。使用人全血测定法（HWBL）对这些混合物进行白三烯B4抑制活性筛选，得到了一种先导化合物1-(6-丁氧基-2-萘基)-3-(4-硝基苯基)丙-2-烯-1-酮（K4A3），其IC50值为18.5微摩尔。
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