Abstract
Objective: In modern years, the biggest dare is to develop new chemotherapeutic agents with high efficiency as well as low toxicity. Hence, to defeat this challenge, extensive endeavors were taken on thiosemicarbazone based metal complexes.
 Methods: A sequence of nine thiosemicarbazone based diimine copper(II) complexes derived from three sulfur-containing ligands N-methyl-2- ((1-methyl-1H-pyrrol-2-yl)methylene)hydrazinecarbothioamide H(L1), N-ethyl-2-((1-methyl-1H-pyrrol-2-yl)methylene)hydrazinecarbothioamide H(L2), and N-benzyl-2-((1-methyl-1H-pyrrol-2-yl)methylene)hydrazinecarbothioamide H(L3). The molecular structures and coordination possibilities of thiosemicarbazone ligands toward the central metal ions have been validated by analytical and spectral techniques such as molar conductance, elemental analysis, ultraviolet–Vis, Fourier-transform infrared, and electron paramagnetic resonance spectroscopy confirms that the thiosemicarbazones ligands are coordinated to copper through NS’ donor and NN’ donor of diimine. The antimicrobial activity and DNA cleavage effectiveness of thiosemicarbazone derivatives and copper(II) complexes were assessed by disc diffusion and agarose gel electrophoresis methods.
 Results: All the spectral studies authenticated that the square planar geometry of the thiosemicarbazone copper(II) complexes 1–9. From the results of antibacterial activity against selected Gram-positive (Bacillus thuringiensis) and Gram-negative (Escherichia coli) bacterial strains, complex 8 exhibited noteworthy activity. Interestingly, copper(II) complexes bearing 1,10-phenanthroline (phen) moiety displayed outstanding results together with N(4)-substituted thiosemicarbazone derivatives and causes complete DNA degradation of SC (supercoiled) pUC18 DNA.
 Conclusion: A variety of substitutions at the thioamide nitrogen atoms have shown potential biological activity. Henceforth, N(4)-substituted thiosemicarbazone based copper(II) complexes virtually reach the effectiveness of conventional chemotherapeutic drugs.
Highlights
Cancer is one of the world’s top killer diseases and it has overtaken heart disease according to 2010 reports, which should be more than higher and causes lots of deaths by 2030
The mixed N/S donors of thiosemicarbazone ligands derived from the combination of an aldehyde or ketone and these groups of ligands are useful for achieving coordination spheres of transition metal complexes
Electronic spectra The UV-Vis measurement of the synthesized thiosemicarbazone ligands and their copper(II) complexes in the 1×10−3M concentration in Dimethyl formamide (DMF) was performed in the wavelength range 200–1000 nm
Summary
Cancer is one of the world’s top killer diseases and it has overtaken heart disease according to 2010 reports, which should be more than higher and causes lots of deaths by 2030. The mixed N/S donors of thiosemicarbazone ligands derived from the combination of an aldehyde or ketone and these groups of ligands are useful for achieving coordination spheres of transition metal complexes. These ligands and their metal complexes have received the extensive notice due to their availability of variable bonding modes, an electron donor’s property of ligand, the position of a ligand inside the coordination sphere, structural variety, ion sensing capability, potential biological applications, and the stability of ligands and complexes [3,4]. Phenyl and ethyl substituted thiosemicarbazone ligands were prepared This was the first report which proved the biological properties of the mixed ligand thiosemicarbazone copper(II) complexes. It is hoped that this work will be afforded some potential biological properties of mixed ligand thiosemicarbazone copper(II) complexes
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