Design and synthesis of threading intercalators to target DNA.

Authors :: Howell LA
Gulam R
Mueller A
O'Connell MA
Searcey M
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Dec 01; Vol. 20 (23), pp. 6956-9. Date of Electronic Publication: 2010 Oct 07.
Publication Year :: 2010
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.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)