Abstract

Four complexes, [Cu2(glyha)(bpy)2(H2O)]·2ClO4·H2O (1), [Cu2(glyha)(phen)2]·2ClO4 (2), [Cu2(alaha)(bpy)2Cl]·Cl·4H2O (3), and [{Cu2(alaha)(phen)2}{Cu2(alaha)(phen)2(NO3)}]·3NO3 (4) (glyha2− = dianion glycinehydroxamic acid, alaha2− = dianion alaninehydroxamic acid, bpy = 2,2′-bipyridine, phen = 1,10-phenanthroline) have been successfully synthesized and characterized by X-ray single crystal diffraction. The interactions of these complexes with calf thymus DNA (CT-DNA) were studied through UV spectroscopy, fluorescence spectroscopy, and circular dichroism. The results revealed that complexes 1–4 could interact with CT-DNA through intercalation. Interactions of all complexes with bovine serum albumin (BSA) were confirmed by the docking study to quench the intrinsic fluorescence of BSA in a static quenching process. Furthermore, the in vitro cytotoxic effect of the complexes was also examined on four tumor cell lines, including human lung carcinoma cell line (A549), human colon carcinoma cell line (HCT-116), human promyelocytic leukemia cell (HL-60) and cervical cancer cell line (HeLa). All complexes exhibited different antitumor activities.

Highlights

  • IntroductionA bad disease, affects modern life and has a high mortality rate. Many of complexes have been found to be active in the restrained reproduction of cancer cells [1,2,3,4,5], and some of them have been used in clinical treatments

  • Cancer, a bad disease, affects modern life and has a high mortality rate

  • DNA, we investigated the mode and the propensity for binding of the higher cytotoxicities of the four complexes with DNA through UV-Vis absorption, fluorescence, and circular dichroism (CD) techniques

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Summary

Introduction

A bad disease, affects modern life and has a high mortality rate. Many of complexes have been found to be active in the restrained reproduction of cancer cells [1,2,3,4,5], and some of them have been used in clinical treatments. Metal complexes with high anticancer activity and non-covalent DNA or protein binding properties have played an important role in antitumor chemotherapy and developed an active research area in metal-based drugs [6]. DNA is the most important target for antitumorals because of its central role in replication and transcription. Considerable attempts are being made to research the interaction of copper(II) complexes with DNA and BSA [7]. Copper complexes can be reacted with DNA by non-covalent binding methods [9]. They exhibited the most potent antitumor activities, and have more effective than cisplatin in vitro tests in some cases [8]. Some complexes involving aminohydroxamic acid ligands show interesting bioactivity [10,11]

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