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. A large number of arylalkyl ketones, benzophenones, desoxybenzoins and chalcones as well as their analogs (54 in total) were 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 a possible mechanism of their ICAM-1 inhibitory activities. The most active compound was found to be 79.
Original language | English (US) |
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Pages (from-to) | 368-377 |
Number of pages | 10 |
Journal | Archiv der Pharmazie |
Volume | 345 |
Issue number | 5 |
DOIs | |
State | Published - May 2012 |
Externally published | Yes |
Keywords
- Arylalkyl ketones
- Benzophenones
- Chalcones
- Desoxybenzoins
- Endothelial cells
- ICAM-1
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery