Nitroreductase-activated nitric oxide (NO) prodrugs

Please use this identifier to cite or link to this item: http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/1588

Title:	Nitroreductase-activated nitric oxide (NO) prodrugs
Authors:	Sharma, Kavita SENGUPTA, KUNDAN CHAKRAPANI, HARINATH Dept. of Chemistry
Keywords:	Nitric oxide Prodrug Nitroreductase Diazeniumdiolate Directed prodrug therapy 2013
Issue Date:	Nov-2013
Publisher:	Elsevier B.V.
Citation:	Bioorganic and Medicinal Chemistry Letters, 23(21), 5964-5967.
Abstract:	Due to the involvement of nitric oxide (NO) in numerous and diverse physiological processes, site-directed delivery of therapeutic NO in order to minimize unwanted side-effects is necessary. O2-(4-Nitrobenzyl) diazeniumdiolates are designed as substrates for Escherichia coli nitroreductase (NTR), an enzyme that is frequently used to facilitate directed delivery of cytotoxic species to cancers. O2-(4-Nitrobenzyl) diazeniumdiolates are found to be stable in aqueous buffer but are metabolized by NTR to produce NO. A cell viability assay revealed that cytotoxic effects of O2-(4-nitrobenzyl)1-(2-methylpiperidin-1-yl)diazen-1-ium-1,2-diolate (4b) towards two cancer cell lines is significantly enhanced in the presence of NTR suggesting the potential for use of this compound in nitric oxide-based directed prodrug therapy.
URI:	http://dr.iiserpune.ac.in:8080/xmlui/handle/123456789/1588 https://doi.org/10.1016/j.bmcl.2013.08.066
ISSN:	0960-894X 1464-3405
Appears in Collections:	JOURNAL ARTICLES

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