Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1 expression on human endothelial cells

Shashwat Malhotra, Sakshi Balwani, Ashish Dhawan, Brajendra K. Singh, Sarvesh Kumar, Rajesh Thimmulappa, Shyam Biswal, Carl E. Olsen, Erik Van Der Eycken, Ashok K. Prasad, Balaram Ghosh, Virinder S. Parmar

Research output: Contribution to journalArticle

Abstract

Novel N-protected derivatives of substituted isatins have been synthesized and evaluated for their potency in inhibiting TNF-α-induced ICAM-1 activity on human endothelial cells as a marker for anti-inflammatory activity. Compound 3p was found to be most potent in inhibiting the ICAM-1 expression in a concentration- and time-dependent manner. The structure-activity relationship of these compounds in inhibiting ICAM-1 expression activity is elucidated in the present study.

Original languageEnglish (US)
Pages (from-to)743-751
Number of pages9
JournalMedChemComm
Volume2
Issue number8
DOIs
StatePublished - Aug 1 2011

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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    Malhotra, S., Balwani, S., Dhawan, A., Singh, B. K., Kumar, S., Thimmulappa, R., Biswal, S., Olsen, C. E., Van Der Eycken, E., Prasad, A. K., Ghosh, B., & Parmar, V. S. (2011). Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1 expression on human endothelial cells. MedChemComm, 2(8), 743-751. https://doi.org/10.1039/c0md00262c