article · Applied Organometallic Chemistry
A novel azo pyrazolone ligand, designated HL, was synthesised alongside its nickel(II), palladium(II), and platinum(II) complexes, with molecular structures validated through spectroscopic techniques, thermal analysis, and density functional theory modelling. Biological assessments focused on the antitumour, antioxidant, antimicrobial, and DNA cleavage characteristics of each compound. Cytotoxicity testing across four tumour cell lines showed that the HL ligand displayed potent activity compared to the reference drug 5-fluorouracil, whilst the palladium(II) complex proved the most effective among the metal coordinates, followed by nickel(II) and platinum(II). The ligand also exhibited higher antioxidant action than the metal complexes. Antimicrobial screenings indicated moderate to high antibacterial effects across all compounds, though only the palladium(II) complex exhibited antifungal activity. Gel electrophoresis demonstrated negligible nuclease action, indicating that antitumour effects stem from interfering with DNA replication rather than direct DNA cleavage.
Finding new compounds to treat tumours remains an urgent priority in medicine. By demonstrating strong cytotoxicity against cancer cell lines whilst protecting DNA from direct cleavage, these synthesised compounds point towards alternative mechanisms for halting tumour replication. This research provides medicinal chemists with promising foundational structures for designing next-generation therapeutic agents that combine antitumour and antioxidant capabilities.
This work is at an early research stage, offering potential value to pharmaceutical companies and academic drug discovery teams pursuing novel oncology therapeutics. The ligand and its palladium complex serve as prospective starting points for designing antitumour agents that interfere with DNA replication. Real-world application remains distant, as extensive formulation work, animal testing, and preclinical toxicology are required to assess safety and therapeutic efficacy beyond these initial laboratory assays.
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The absolute necessity to fight some class of tumor is perceived as serious health concerns, so the discovery and development of effective anticancer agents are urgently needed. ( E )‐4‐((2‐hydroxyphenyl)diazenyl)‐3‐phenyl‐1 H ‐pyrazol‐5(4 H )‐one, HL, and its Ni(II), Pd(II) and Pt(II) complexes were synthesized and the biological activity was evaluated for antitumor, antioxidant and antimicrobial activity as well as DNA cleavage. Their structures were assigned depending on the elemental analysis, conductivity, magnetic moment, spectral measurements (IR, 1 HNMR, mass and UV–Vis) and thermal analysis. 3D molecular modeling using DFT method confirmed that the geometrical structures agree well with the suggested experimental ones. The antitumor activity was evaluated against four different cell lines using MTT assay. The ligand HL showed a potent cytotoxic activity compared to 5‐fluorouracil as a reference drug. For metal complexes, the order of activity was: Pd(II) > Ni(II) > Pt(II). A remarkable antioxidant activity for the ligand HL was recorded. It was higher than that of the metal complexes. Results of antimicrobial experiments revealed that all compounds were moderate to highly active against selected bacterial strains but inactive as antifungal except Pd(II) which showed a moderate antifungal activity. Gel electrophoresis showed insignificant nucleases activity for the ligand or its metal complexes even in the presence of H 2 O 2 providing protection of DNA from damage. The antitumor activity of our compounds may be not due to DNA cleavage but may be referred to a mechanism similar to that of 5‐fluorouracil which interfere with DNA replication. The present work suggests the use of this ligand in the design and development of new anticancer drugs.
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DOI: 10.1002/aoc.4104
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