Arylalkyl Ketones, Benzophenones, Desoxybenzoins and Chalcones Inhibit TNF-a Induced Expression of ICAM-1: Structure-Activity Analysis

作者：Kumar Sarvesh; Reddy Chandra Shekhar L; 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

来源：Archiv der Pharmazie, 2012, 345(5): 368-377.

DOI：10.1002/ardp.201100279

• Arylalkyl ketones
• Benzophenones
• Chalcones
• Desoxybenzoins
• Endothelial cells
• ICAM-1

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.

• 出版日期2012-5