Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 5, Pages 1969-1975Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.038
Keywords
Inflammation; 5-Lipoxygenase; One-pot multicomponent reaction; Arachidonic acid cascade; Allergic diseases
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Funding
- LOEWE Lipid Signaling Forschungszentrum Frankfurt (LiFF)
- Oncogenic Signaling Frankfurt (OSF)
- EU [LSHM-CT-2004-0050333]
- Fonds der Chemischen Industrie
- DAAD-La Caixa (Spain)
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A novel class of 5-lipoxygenase (5-LO) inhibitors characterized by a central imidazo[1,2-a] pyridine scaffold, a cyclohexyl moiety and an aromatic system, is presented. This scaffold was identified in a virtual screening study and exhibits promising inhibitory potential on the 5-LO. Here, we investigate the structure-activity relationships of this compound class. With N-cyclohexyl-6-methyl-2-(4-morpholinophenyl)imidazo[1,2-a]pyridine-3-amine (14), we identified a potent 5-LO inhibitor (IC50 = 0.16 mu M (intact cells) and 0.1 mu M (cell-free)), which may possess potential as an effective lead compound intervening with inflammatory diseases and certain types of cancer. (C) 2012 Elsevier Ltd. All rights reserved.
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