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, 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

Bloomberg School of Public Health

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

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 language	English (US)
Pages (from-to)	743-751
Number of pages	9
Journal	MedChemComm
Volume	2
Issue number	8
DOIs	https://doi.org/10.1039/c0md00262c
State	Published - Aug 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

Malhotra, S, Balwani, S, Dhawan, A, Singh, BK, Kumar, S, Thimmulappa, R, Biswal, S, Olsen, CE, Van Der Eycken, E, Prasad, AK, Ghosh, B & Parmar, VS 2011, 'Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1 expression on human endothelial cells', MedChemComm, vol. 2, no. 8, pp. 743-751. https://doi.org/10.1039/c0md00262c

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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.",

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year = "2011",

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doi = "10.1039/c0md00262c",

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AU - Balwani, Sakshi

AU - Dhawan, Ashish

AU - Singh, Brajendra K.

AU - Kumar, Sarvesh

AU - Thimmulappa, Rajesh

AU - Biswal, Shyam

AU - Olsen, Carl E.

AU - Van Der Eycken, Erik

AU - Prasad, Ashok K.

AU - Ghosh, Balaram

AU - Parmar, Virinder S.

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AB - 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.

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

Abstract

ASJC Scopus subject areas

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