Synthesis, DNA-cleaving activities and cytotoxicities of the copper(II) complexes of pyrrole-polyamide dimers tethered with carboxylate-containing linkers

• Two Cu(II) complexes were synthesized from dimeric mono- and dipyrrole-polyamides.
• Both complexes efficiently cleaved DNA, presumably via an oxidative mechanism.
• Complex 2 exhibited higher overall catalytic efficiency (kmax/KM) than complex 1.
• Both complexes showed moderate inhibitory activities toward HepG2 and A549 cells.

This paper describes the synthesis of two new Cu(II) complexes, that is, complexes 1 and 2, from dimeric monopyrrole-polyamide L1 and dipyrrole-polyamide L2 tethered with carboxylate-containing linkers, respectively. These two complexes were found to be capable of efficiently converting pBR322 DNA into open circular and linear forms under physiological conditions, presumably via an oxidative mechanism. Kinetic assays indicate that, compared with complex 1, complex 2 exhibited higher DNA-binding affinity and overall catalytic activity (kmax/KM). In addition, both complexes showed moderate inhibitory activities toward HepG2 and A549 cells.

Two new Cu(II) complexes were synthesized from dimeric mono- and dipyrrole-polyamides tethered with carboxylate-containing linkers and found to exhibit high DNA-cleaving activities under physiological conditions, presumably via an oxidative mechanism. In addition, both complexes showed moderate inhibitory activities toward HepG2 and A549 cells.Figure optionsDownload as PowerPoint slide