Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: Inhibitors of leukotriene B-4

Authors
Deshpande, AM Argade, NP Natu, AA Eckman, J
Citation
Am. Deshpande et al., Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: Inhibitors of leukotriene B-4, BIO MED CH, 7(6), 1999, pp. 1237-1240
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
6
Year of publication
1999
Pages
1237 - 1240
Database
ISI
SICI code
0968-0896(199906)7:6<1237:SASOAC>2.0.ZU;2-O
Abstract
A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leuko triene 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.