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

International Journal of Molecular Sciences
Mohamed F AlAjmiRais Ahmad Khan

Abstract

Herein, we have synthesized and characterized a new benzimidazole-derived "BnI" ligand and its copper(II) complex, [Cu(BnI)₂], 1, and zinc(II) complex, [Zn(BnI)₂], 2, using elemental analysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the biomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration, fluorescence techniques, and in silico molecular docking studies. The results exhibited the significant binding propensity of both complexes 1 and 2, but complex 1 showed more avid binding to HSA and DNA. Also, the nuclease activity of 1 and 2 was analyzed for pBR322 DNA, and the results obtained confirmed the potential of the complexes to cleave DNA. Moreover, the mechanistic pathway was studied in the presence of various radical scavengers, which revealed that ROS (reactive oxygen species) are responsible for the nuclease activity in complex 1, whereas in complex 2, the possibility of hydrolytic cleavage also exists. Furthermore, the cytotoxicity of the ligand and complexes 1 and 2 were studied on a panel of five different human cancer cells, namely: HepG2, SK-MEL-1, HT018, HeLa, and MDA-MB 231, and compared with the standard drug, cisplatin. The results are quite pro...Continue Reading

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Citations

Jun 23, 2019·Journal of Biomolecular Structure & Dynamics·Amer M AlanaziMohammad Hassan Baig
Jun 4, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ihsan A ShehadiMonther A Khanfar
Dec 6, 2018·International Journal of Molecular Sciences·Christina N Banti, Sotiris K Hadjikakou
Dec 16, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Marina PorchiaCarlo Santini

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Methods Mentioned

BETA
X-ray
NMR
FRET
Assay
flow cytometry
FCS

Software Mentioned

Discovery Studio
Hex
Autodock4
AutoDockTool
AutoGrid
Autodock

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