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

This paper describes the synthesis of two new Cu(II) complexes, that is, complexes 1 and 2, from dimeric monopyrrole-polyamide L-1 and dipyrrole-polyamide L-2 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 (k(max)/K-M). In addition, both complexes showed moderate inhibitory activities toward HepG2 and A549 cells. (C) 2015 Elsevier B.V. All rights reserved.