Arylalkyl ketones, benzophenones, desoxybenzoins and chalcones inhibit TNF-α induced expression of ICAM-1: Structure-activity analysis

Sarvesh Kumar, Chandra Shekhar Reddy L, Yogesh Kumar, Amit Kumar, Brajendra K. Singh, Vineet Kumar, Shashwat Malhotra, Mukesh K. Pandey, Rajni Jain, Rajesh Thimmulappa, Sunil K. Sharma, Ashok K. Prasad, Shyam Biswal, Erik Van Der Eycken, Anthony L. Depass, Sanjay V. Malhotra, Balaram Ghosh, Virinder S. Parmar

Research output: Contribution to journalArticle

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 languageEnglish (US)
Pages (from-to)368-377
Number of pages10
JournalArchiv der Pharmazie
Volume345
Issue number5
DOIs
StatePublished - May 2012

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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  • Cite this

    Kumar, S., Reddy L, C. S., Kumar, Y., Kumar, A., Singh, B. K., Kumar, V., Malhotra, S., Pandey, M. K., Jain, R., Thimmulappa, R., Sharma, S. K., Prasad, A. K., Biswal, S., Van Der Eycken, E., Depass, A. L., Malhotra, S. V., Ghosh, B., & Parmar, V. S. (2012). Arylalkyl ketones, benzophenones, desoxybenzoins and chalcones inhibit TNF-α induced expression of ICAM-1: Structure-activity analysis. Archiv der Pharmazie, 345(5), 368-377. https://doi.org/10.1002/ardp.201100279