Biologically active [Pd2L4]4+ quadruply-stranded helicates: stability and cytotoxicity

摘要: There is emerging interest in the anti-proliferative effects of metallosupramolecular systems due to different size and shape these metallo-architectures compared traditional small molecule drugs. Palladium(II)-containing are most abundant class complexes, yet their biological activity has hardly been examined. Here a series [Pd2(L)4](BF4)4 quadruply-stranded, dipalladium(II) architectures were screened for cytotoxic against three cancer cell lines one non-malignant line. The helicates exhibited range properties, with complex [Pd2(hextrz)4](BF4)4 possessing low micromolar IC50 values all tested, while other displayed moderate or no cytotoxicity. Against MDA-MB-231 line, which resistant platinum-based drugs, was 7-fold more active than cisplatin. Preliminary mechanistic studies indicate that helicate does not induce death same way as clinically used metal complexes such Rather interacting DNA, appears disrupt membrane. These represent first characterisation quadruply-stranded architectures, provide insight into design requirements development biologically stable palladium(II)-containing architectures.