Novel polyamide amidine anthraquinone platinum(II) complexes: cytotoxicity, cellular accumulation, and fluorescence distributions in 2D and 3D cell culture models

1- and 1,5-Aminoalkylamine substituted anthraquinones (AAQs, 1C3 1,5C3) were peptide coupled to 1-, 2-, 3-pyrrole lexitropsins generate compounds that incorporated both DNA minor groove intercalating moieties. The corresponding platinum(II) amidine complexes synthesized through a synthetically facile amine-to-platinum mediated nitrile ‘Click’ reaction. precursors as well the biologically evaluated in 2D monolayer cells 3D tumour cell models. Despite having cellular accumulation levels up five-fold lower than of cisplatin, platinum had cytotoxicities only three-fold lower. Accumulation was lowest for with two or three pyrrole groups, but latter most active exceeding activity cisplatin MDA-MB-231 line. All showed moderate good penetration into spheroids DLD-1 distributions being consistent uptake containing regions starved nutrients.Graphic abstract