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.

引用

页码：1237 / 1240

页数：4

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