Synthesis and screening of a combinatorial library of naphthalene substituted chalcones:: Inhibitors of leukotriene B4

被引：39
作者：
Deshpande, AM
Argade, NP
Natu, AA [1 ]
Eckman, J
机构：
[1] Natl Chem Lab, Div Organ Chem Synth, Poona 411008, Maharashtra, India
[2] CytoMed Inc, Cambridge, MA 02139 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 06期
关键词：
naphthalene chalcones; antiinflammatories; enzyme inhibitors; leukotrienes;
D O I：
10.1016/S0968-0896(99)00047-4
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene Bq 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 (K(4)A(3)) with an IC50 value of 18.5 mu M. (C) 1999 Elsevier Science Ltd. All rights reserved.
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收藏
页码：1237 / 1240
页数：4
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