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
相关论文
共 15 条
  • [1] [Anonymous], 1963, Friedel-Crafts and Related Reactions
  • [2] BROOKS DW, 1993, PERSPECTIVES MED CHE, P119
  • [3] INDAZOLINONES, A NEW SERIES OF REDOX-ACTIVE 5-LIPOXYGENASE INHIBITORS WITH BUILT-IN SELECTIVITY AND ORAL ACTIVITY
    BRUNEAU, P
    DELVARE, C
    EDWARDS, MP
    MCMILLAN, RM
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (03) : 1028 - 1036
  • [4] RESPONSES OF HUMAN-SKIN TO INTRADERMAL INJECTION OF LEUKOTRIENE-C4, LEUKOTRIENE-D4 AND LEUKOTRIENE-B4
    CAMP, RDR
    COUTTS, AA
    GREAVES, MW
    KAY, AB
    WALPORT, MJ
    [J]. BRITISH JOURNAL OF PHARMACOLOGY, 1983, 80 (03) : 497 - 502
  • [5] LEUKOTRIENES ARE POTENT CONSTRICTORS OF HUMAN BRONCHI
    DAHLEN, SE
    HEDQVIST, P
    HAMMARSTROM, S
    SAMUELSSON, B
    [J]. NATURE, 1980, 288 (5790) : 484 - 486
  • [6] COMPARATIVE AIRWAY AND VASCULAR ACTIVITIES OF LEUKOTRIENE-C-1 AND LEUKOTRIENE-D INVIVO AND INVITRO
    DRAZEN, JM
    AUSTEN, KF
    LEWIS, RA
    CLARK, DA
    GOTO, G
    MARFAT, A
    COREY, EJ
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1980, 77 (07): : 4354 - 4358
  • [7] Synthesis and anti-inflammatory activity of chalcone derivatives
    Herencia, F
    Ferrándiz, ML
    Ubeda, A
    Domínguez, JN
    Charris, JE
    Lobo, GM
    Alcaraz, MJ
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (10) : 1169 - 1174
  • [8] Kohler EP, 1922, ORG SYNTH, V2, P1
  • [9] LEUKOTRIENE-B4 AND INFLAMMATORY DISEASE
    MCMILLAN, RM
    FOSTER, SJ
    [J]. AGENTS AND ACTIONS, 1988, 24 (1-2): : 114 - 119
  • [10] ODONNELL M, 1989, THERAPEUTIC APPROACHES TO INFLAMMATORY DISEASES, P169
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