Abstract

Six new zinc(II) complexes were prepared by the reaction of ZnBr2 or ZnI2 with 4′-(substituted-phenyl)-2,2′:6′,2′′-terpyridine compounds, bearing p-methylsulfonyl (L1), p-methoxy (L2) and p-methyl (L3), which were characterized by elemental analysis, FT-IR, NMR and single crystal X-ray diffraction. The antiproliferative properties against Eca-109, A549 and Bel-7402 cell lines and the cytotoxicity test on RAW-264.7 of these compounds were monitored using a CCK-8 assay, and the studies indicate that the complexes show higher antiproliferative activities than cisplatin. The interactions of these complexes with CT-DNA and proteins (BSA) were studied by UV-Vis, circular dichroism (CD) and fluorescent spectroscopy, respectively. The results indicate that the interaction of these zinc(II) complexes with CT-DNA is achieved through intercalative binding, and their strong binding affinity to BSA is fulfilled through a static quenching mechanism. The simulation of the complexes with the CT-DNA fragment and BSA was studied by using molecular docking software. It further validates that the complexes interact with DNA through intercalative binding mode and that they have a strong interaction with BSA.

Highlights

  • Cancer is one of the leading causes of death worldwide, with more than 10 million people suffering from the disease yearly [1,2,3]

  • Complexes 1–6 were characterized by 1 H-NMR spectroscopy (Figures S1–S6, Supplementary Materials), Complexes 1–6 were characterized by 1H-NMR spectroscopy (Figures S1–S6, Supplementary Materials), IR

  • Six new zinc (II) complexes were prepared by the reaction of ZnBr2 or ZnI2 with 40 -(substitutedphenyl)-2,20 :60,200 -terpyridine, which were characterized by elemental analysis, FT-IR, NMR and single crystal X-ray diffraction

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Summary

Introduction

Cancer is one of the leading causes of death worldwide, with more than 10 million people suffering from the disease yearly [1,2,3]. Since its introduction in medical practice, cisplatin has been one of the most effective drugs for the treatment of cancers [4,5,6,7]. The biological activity of cisplatin comes from the fact that its covalent binding with DNA leads to cell death or apoptosis. There are serious side effects such as nephrotoxicity, neurotoxicity, gastrointestinal toxicity, bone marrow suppression and drug resistance [8,9,10], among others. These side effects limit the application of platinum drugs and promote the development of alternative therapeutics [11,12,13]. The production of Molecules 2020, 25, 3459; doi:10.3390/molecules25153459 www.mdpi.com/journal/molecules

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