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

doi:10.1039/C0MD00262C

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

Shashwat Malhotra,^a Sakshi Balwani,^b Ashish Dhawan,^a Brajendra K. Singh,^ac Sarvesh Kumar,^bd Rajesh Thimmulappa,^d Shyam Biswal,^d Carl E. Olsen,^e Erik Van der Eycken,^c Ashok K. Prasad,^a Balaram Ghosh*^b and Virinder S. Parmar*^a

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* Corresponding authors

^a Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi, India
E-mail: virparmar@gmail.com.
Fax: +91-11-27667206
Tel: +91-11-27667206

^b Molecular Immunogenetics Laboratory, CSIR-Institute of Genomics and Integrative Biology, University of Delhi Campus (North), Mall Road, Delhi, India
E-mail: bghosh@igib.res.in.
Fax: +91-11-27667471
Tel: +91-11-27662580

^c Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Katholieke Universiteit Leuven, Celestijnenlaan200F, Leuven, Belgium

^d Department of Environmental Health Sciences, Bloomberg School of Public Health, Johns Hopkins University, Baltimore, Maryland, USA

^e Department of Basic Sciences and Environment, University of Copenhagen, Frederiksberg C, Denmark

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.

MedChemComm

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

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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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