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

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 1999-06, Vol.7 (6), p.1237-1240
Main Authors: DESHPANDE, A. M, ARGADE, N. P, NATU, A. A, ECKMAN, J
Format: Article
Language:English
Subjects:
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Chalcone - chemistry
Drug Evaluation, Preclinical
Humans
Leukotriene Antagonists - chemical synthesis
Leukotriene Antagonists - pharmacology
Leukotriene B4 - antagonists & inhibitors
Leukotriene B4 - metabolism
Medical sciences
Naphthalenes - chemistry
Pharmacology. Drug treatments
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Summary: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.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(99)00047-4