article · Applied Organometallic Chemistry
Researchers synthesised and characterised novel metal complexes using palladium, iron, chromium, nickel, and copper combined with a ciprofloxacin-derived Schiff base ligand known as CFAP. Chemical analyses, stability profiles, and computational calculations established that the ligand binds to the metals in a one-to-one ratio, forming octahedral geometries for most metals and a square planar geometry for the palladium complex. Laboratory testing demonstrated that the compounds possess antioxidant properties and bind effectively to DNA. In evaluations against fungal and bacterial pathogens, the palladium complex exhibited higher antimicrobial efficacy than the reference drugs fluconazole and ofloxacin. Furthermore, screening against liver, breast, and colon cancer cell lines revealed that the palladium complex showed the highest anticancer activity among the tested compounds, performing favourably against the reference drug vinblastine.
Microbial resistance and cancer remain pressing global health challenges that require new therapeutic options. By modifying existing antibiotics into metal complexes, scientists can potentially generate compounds with enhanced and diverse biological activities. These findings show that ciprofloxacin-derived metal complexes can act against bacterial and fungal targets while also displaying antioxidant activity and inhibiting cancer cell lines in preliminary laboratory models.
This research could support the development of novel dual-action antimicrobial and anticancer pharmaceutical formulations. The immediate potential users are medicinal chemists and pharmaceutical drug discovery teams seeking lead molecules. However, the findings represent very early-stage research limited to in vitro laboratory assays, meaning the compounds are far from clinical application and require extensive preclinical toxicology, pharmacokinetic assessment, and in vivo trials before commercial use can be considered.
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ABSTRACT Novel compounds with pharmacological activity were synthesized from Pd(II), Fe(III), Cr(III), Ni(II), and Cu(II) ions with 1‐cyclopropyl‐6‐fluoro‐4‐(2‐hydroxy‐phenylimino)‐7‐piperazin‐1‐yl‐1,4‐dihydro‐quinoline‐3‐carboxylic acid (CFAP). The ligand's NH and OH groups allowed it to interact with the metals as a neutral tridentate. The investigated novel compounds were described using 1 H and 13 C NMR spectra, FT‐IR spectrums, TGA and UV–Vis (conductance of molecules), and CHN‐analysis. Additionally, the pH profile of the CFAP complexes indicated great stability, and the complexes' stability constant was discovered in the solution. To extract important properties for CFAP and its complexes, computational research was used, CFAPCu, CFAPCr, CFAPNi, and CFAPFe have octahedral geometry, while CFAPPd has square planar geometry. To investigate the molecular geometry, density functional theory calculations (DFT) were carried out. The molar ratio and continuous fluctuation data confirmed that the (M:L) ratio was (1:1). In vitro tests were conducted to evaluate Schiff base's antimicrobial action ligand and its metal chelates against fungal and bacterial infections. The findings showed that the antimicrobial efficacy is as follows: When CFAPPd is compared to fluconazol and ofloxacin as reference medications, it is the highly inhibitor complex. The novel CFAP ligand and its complexes were investigated for In vitro carcinogenic potential against Hep‐G2, MCF‐7, and HCT‐116 cell lines. As compared to the medication vinblastine, the results once again demonstrated that CFAPPd is the most active agent. Moreover, the complexes demnstrated strong reactivity in capturing free radicals when their antioxidant activity was investigated. Viscosity, spectral investigations, and gel electrophoreses were used to identify the interaction between metal chelates and DNA. Every examined compound is shown to be an enthusiastic DNA binder by viscosity and spectrophotometric titration investigations. The heightened hydrophobic and electrostatic interactions between aromatic rings could be the cause of this. Ultimately, these compounds could be regarded as promising bioactive substances.
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DOI: 10.1002/aoc.7667
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