Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1 expression on human endothelial cells
Malhotra, Shashwat × Balwani, Sakshi Dhawan, Ashish Singh, Brajendra K Kumar, Sarvesh Thimmulappa, Rajesh Biswal, Shyam Olsen, Carl E Van der Eycken, Erik Prasad, Ashok K Ghosh, Balaram Parmar, Virinder S #
Novel N-protected derivatives of substituted isatins have been synthesized and evaluated for their potency in inhibiting TNF-alpha-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.