Evaluating anticancer activity and DNA-binding properties ofcycloplatinated (II) water-soluble complexes

According to WHO, cancer is the second leading cause of diseases globally and is responsiblefor an evaluated ۹.۶ million deaths in ۲۰۱۸ [۱]. Universally, about ۱ in ۶ deaths is because ofcancer [۲]. New anticancer chemotherapeutics, that can effectively cure this disease with minimalside effects, maintain initial importance to the world research community [۳]. In this study, fourPt-based complexes, [Pt (N^C) (CN) (L)], and [Pt (N^C) (CN)۲], in which N^C = deprotonated ۲-phenyl pyridine (ppy) or benzo[h]quinoline (bhq), and L = p-Tolyl or methyl were synthesized[۴,۵]. These complexes are characterized by NMR spectroscopy. In addition, the biomolecularinteractions of complexes with calf-thymus DNA (CT-DNA) and ethidium bromide (EB) arestudied by fluorescence spectroscopy and UV−vis measurements. The potential of Pt complexes(C۱–C۴) to use as an anticancer agent and their cytotoxicity against MCF-۷, A۵۴۹, HT۲۹, andMDA-MB-۲۳۱ cancer cell lines were measured by using ۳-(۴, ۵-dimethylthiazol-۲-yl)-۲, ۵-diphenyl tetrazolium bromide (MTT) assay. To better understand the nature of the binding, acompetitive assay between the complexes and ethidium bromide for DNA binding was studied.According to the results obtained from these analyses, [Pt(ppy)(CN)(p-Tolyl)] has morecytotoxicity for MCF-۷, A۵۴۹, and HT۲۹ cancer cell lines, also, [Pt(bzq)(CN)(p-Tolyl)] has morecytotoxicity for MDA-MB-۲۳۱ cancer cell lines. Overall, the present work suggests that acontrolled modification could result in new potential antitumor complexes which can survive therepair mechanism and induce facile apoptosis. It can be concluded that the cyclomatalatedplatinum(II) complexes are highly promising leads for the development of novel effective DNAtargetedanticancer drugs.