Bisintercalator natural products with potential therapeutic applications: isolation, structure determination, synthetic and biological studies

Dawson, S., Malkinson, J.P., Paumier, D. and Searcey, M. (2007) Bisintercalator natural products with potential therapeutic applications: isolation, structure determination, synthetic and biological studies. Natural Product Reports, 24 (1). pp. 109-126. 10.1039/b516347c.

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DOI: 10.1039/b516347c

Abstract

Echinomycin is the prototypical bisintercalator, a molecule that binds to DNA by inserting two planar chromophores between the base-pairs of duplex DNA, placing its cyclic depsipeptide backbone in the minor groove. As such, it has been the focus of an extensive number of investigations into its biological activity, nucleic acid binding and, to some extent, its structure-activity relationships. However, echinomycin is also the parent member of an extended family of natural products that interact with DNA by a similar mechanism of bisintercalation. The structural variety in these compounds leads to changes in sequence selectivity and and biological activity, particularly as anti-tumour and anti-viral agents. One of the more recently identified marine natural products that is moving close to clinical development is thiocoraline, and it therefore seems timely to review the various bisintercalator natural products.

Item Type:Article
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2400
Journal or Publication Title:Natural Product Reports
Deposited By:Library Staff
Deposited On:03 Nov 2011 16:49
Last Modified:03 Nov 2011 16:49

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