DNA threading agents: Effect of sidechain bulk on DNA binding and cytotoxicity of 9-anilinoacridine-4-carboxamides

Searcey, Mark ORCID: https://orcid.org/0000-0003-2273-8949, Martin, P. Noel, Howarth, Nicola M., Madden, Bernie and Wakelin, Laurence P. G. (1996) DNA threading agents: Effect of sidechain bulk on DNA binding and cytotoxicity of 9-anilinoacridine-4-carboxamides. Bioorganic and Medicinal Chemistry Letters, 6 (15). pp. 1831-1836. ISSN 0960-894X

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Abstract

A series of 9-anilinoacridine-4-carboxamides with cycloalkyl sidechains has been synthesised to study the effect of sidechain bulk on the DNA binding properties and biological activity of these potential threading intercalators. With sidechains larger than cyclohexane the pKa of the acridine is exceptionally low, so that DNA binding is restricted to pHs below 5. The compounds are cytotoxic to human colon carcinoma cells in the μM range irrespective of their ability to bind to DNA.

Item Type:	Article
Uncontrolled Keywords:	biochemistry,molecular medicine,molecular biology,pharmaceutical science,drug discovery,clinical biochemistry,organic chemistry ,/dk/atira/pure/subjectarea/asjc/1300/1303
Related URLs:	http://www.scopus.com/inward/record.url?...
Depositing User:	LivePure Connector
Date Deposited:	03 Oct 2022 12:32
Last Modified:	25 Oct 2022 00:15
URI:	https://ueaeprints.uea.ac.uk/id/eprint/88820
DOI:	10.1016/0960-894X(96)00325-3

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