Design and synthesis of threading intercalators to target DNA

Howell, Lesley, Gulam, Rosul, Mueller, Anja ORCID: https://orcid.org/0000-0003-0774-0434, O'Connell, Maria ORCID: https://orcid.org/0000-0002-0267-0951 and Searcey, Mark ORCID: https://orcid.org/0000-0003-2273-8949 (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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Abstract

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 (former - to 2024)
UEA Research Groups:	Faculty of Science > Research Groups > Pharmaceutical Cell Biology (former - to 2017) Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017) Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021) Faculty of Science > Research Groups > Molecular and Tissue Pharmacology
Depositing User:	Rachel Smith
Date Deposited:	17 Mar 2011 10:20
Last Modified:	24 Sep 2024 09:08
URI:	https://ueaeprints.uea.ac.uk/id/eprint/26463
DOI:	10.1016/j.bmcl.2010.09.128

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