Heteroleptic Copper(I) Complexes of “Scorpionate” Bis-pyrazolyl Carboxylate Ligand with Auxiliary Phosphine as Potential Anticancer Agents: An Insight into Cytotoxic Mode

Abstract

New copper(I) complexes [CuCl(PPh3)(L)] (1: L = LA = 4-carboxyphenyl)bis(3,5-dimethylpyrazolyl)methane; (2: L = LB = 3-carboxyphenyl)bis(3,5-dimethylpyrazolyl)methane) were prepared and characterised by elemental analysis and various spectroscopic techniques such as FT-IR, NMR, UV–Vis, and ESI-MS. The molecular structures of complexes 1 and 2 were analyzed by theoretical B3LYP/DFT method. Furthermore, in vitro DNA binding studies were carried out to check the ability of complexes 1 and 2 to interact with native calf thymus DNA (CT-DNA) using absorption titration, fluorescence quenching and circular dichroism, which is indicative of more avid binding of the complex 1. Moreover, DNA mobility assay was also conducted to study the concentration-dependent cleavage pattern of pBR322 DNA by complex 1, and the role of ROS species to have a mechanistic insight on the cleavage pattern, which ascertained substantial roles by both hydrolytic and oxidative pathways. Additionally, we analyzed the potential of the interaction of complex 1 with DNA and enzyme (Topo I and II) with the aid of molecular modeling. Furthermore, cytotoxic activity of complex 1 was tested against HepG2 cancer cell lines. Thus, the potential of the complex 1 is promising though further in vivo investigations may be required before subjecting it to clinical trials.

Design, Synthesis, and Biological Evaluation of Benzimidazole-Derived Biocompatible Copper(II) and Zinc(II) Complexes as Anticancer Chemotherapeutics

“…The standard protocol [ 32 ] was adopted for both the experiments, with the slight modifications that we reported earlier [ 36 , 37 , 38 , 39 , 40 ].…”

Biological evaluation of dinuclear copper complex/dichloroacetic acid cocrystal against human breast cancer: design, synthesis, characterization, DFT studies and cytotoxicity assays

“…In vitro experiment on MCF7 (human, mammary gland, metastatic site, epithelial cell, breast cancer) cell line viz., cell proliferation, cell culture, MTT assay, AO/EB staining and ROS generation assays were carried by adopting standard methods [77][78][79] with slight modication as reported earlier by us and references therein. [80][81][82][83][84][85] The cell lines was purchased from ATCC.…”

Towards anticancer fluoroquinolones: A review article

“…Metal ion complexes have a great interest in medicinal chemistry and were generally reported to have a value in cell growth inhibition and anticancer activity . On the other hand, quinolones were hypothesized to exert their activity via formation of ternary complex with DNA and enzyme mediated by Mg +2 ion .…”