TY - JOUR
T1 - Design and synthesis of threading intercalators to target DNA
AU - Howell, Lesley
AU - Gulam, Rosul
AU - Mueller, Anja
AU - O'Connell, Maria
AU - Searcey, Mark
PY - 2010/10/7
Y1 - 2010/10/7
N2 - 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.
AB - 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.
U2 - 10.1016/j.bmcl.2010.09.128
DO - 10.1016/j.bmcl.2010.09.128
M3 - Article
VL - 1
SP - 6956
EP - 6959
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 20
ER -