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Issue 8, 2011
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Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1 expression on human endothelial cells

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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.

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

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Publication details

The article was received on 15 Dec 2010, accepted on 06 May 2011 and first published on 17 Jun 2011


Article type: Concise Article
DOI: 10.1039/C0MD00262C
Med. Chem. Commun., 2011,2, 743-751

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

    S. Malhotra, S. Balwani, A. Dhawan, B. K. Singh, S. Kumar, R. Thimmulappa, S. Biswal, C. E. Olsen, E. Van der Eycken, A. K. Prasad, B. Ghosh and V. S. Parmar, Med. Chem. Commun., 2011, 2, 743
    DOI: 10.1039/C0MD00262C

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