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From multiply active natural product to candidate drug? Antibacterial (and other) minor groove binders for DNA

Suckling, Colin (2012) From multiply active natural product to candidate drug? Antibacterial (and other) minor groove binders for DNA. Future Medicinal Chemistry, 4 (8). pp. 971-989. ISSN 1756-8919

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Abstract

Natural products that bind to DNA in the minor groove are valuable templates for drug design. Examples include distamycin, netropsin, duocarmycin and anthramycin. Anticancer and anti-infective drugs feature strongly amongst their derivatives. The structures and activities of chemotypes with various therapeutic actions are discussed in the context of the broader field of therapeutically active minor groove binders. The evolution of a series of exceptionally potent and nontoxic antibacterial compounds is discussed using the general design principle of introducing additional hydrophobicity into the distamycin template to increase the strength of binding to DNA. As well as potent antibacterial compounds, antifungal and antiparasitic compounds with exceptional cellular activity against trypanosomes have been identified. Possible mechanisms of action including gene regulation and topoisomerase inhibition are discussed with the need in mind to understand selective toxicity in the series to support future drug discovery.

Item type: Article
ID code: 40340
Keywords: gram positive bacteria, resistant staphylococcus aureus, substituted thiazole polyamide, pyrrole imidazole polyamides, inverted CCAAT BOX-2, sequence recognition, antitumor activity, plasmodium-falciparum, molecular recognition, Chemistry, Pharmacology, Molecular Medicine, Drug Discovery
Subjects: Science > Chemistry
Department: Faculty of Science > Pure and Applied Chemistry
Related URLs:
Depositing user: Pure Administrator
Date Deposited: 04 Jul 2012 10:06
Last modified: 27 Mar 2014 10:15
URI: http://strathprints.strath.ac.uk/id/eprint/40340

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