Design and synthesis of threading intercalators to target DNA

Howell, Lesley, Gulam, Rosul, Mueller, Anja ORCID:, O'Connell, Maria ORCID: and Searcey, Mark ORCID: (2010) Design and synthesis of threading intercalators to target DNA. Bioorganic & Medicinal Chemistry Letters, 1 (20). pp. 6956-6959. ISSN 1464-3405

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Threading intercalators are high affinity DNA binding agents that bind by inserting a chromophore into the duplex and locating one group in each groove. The first threading intercalators that can be conjugated to acids, sulfonic acids and peptides to target them to duplex DNA are described, based upon the well studied acridine-3- or 4-carboxamides. Cellular uptake of the parent acridine is rapid and it can be visualized in the nucleus of cells. Both the parent compounds and their conjugates maintain antitumor activity.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
Depositing User: Rachel Smith
Date Deposited: 17 Mar 2011 10:20
Last Modified: 23 Oct 2022 01:11
DOI: 10.1016/j.bmcl.2010.09.128

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