Title: Arylalkyl Ketones, Benzophenones, Desoxybenzoins and Chalcones Inhibit TNF-α Induced Expression of ICAM-1: Structure-Activity Analysis
Authors: Kumar, Sarvesh ×
Reddy L, Chandra Shekhar
Kumar, Yogesh
Kumar, Amit
Singh, Brajendra K
Kumar, Vineet
Malhotra, Shashwat
Pandey, Mukesh K
Jain, Rajni
Thimmulappa, Rajesh
Sharma, Sunil K
Prasad, Ashok K
Biswal, Shyam
Van der Eycken, Erik
Depass, Anthony L
Malhotra, Sanjay V
Ghosh, Balaram
Parmar, Virinder S #
Issue Date: May-2012
Publisher: VCH Verlagsgesellschaft mbH
Series Title: Archiv der Pharmazie vol:345 issue:5 pages:368-377
Abstract: The interaction between leukocytes and the vascular endothelial cells (EC) via cellular adhesion molecules plays an important role in the pathogenesis of various inflammatory and autoimmune diseases. Small molecules that block these interactions have been targeted as potential therapeutic agents against acute and chronic inflammatory diseases. In an effort to identify potent intercellular cell adhesion molecule-1 (ICAM-1) inhibitors, a large number of arylalkyl ketones, benzophenones, desoxybenzoins and chalcones and their analogs (54 in total) have been synthesized and screened for their ICAM-1 inhibitory activity. The structure-activity relationship studies of these compounds identified three potent chalcone derivatives and also demonstrated the possible mechanism for their ICAM-1 inhibitory activities. The most active compound was found to be 79.
ISSN: 0365-6233
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Design and Synthesis
× corresponding author
# (joint) last author

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