What question did this study set out to answer?

This research aims to synthesize and characterize new platinum(II) complexes with selenone ligands to evaluate their potential as cancer inhibitors.

April 22, 2026Journal of King Saud University - Science0 citationsOpen Access

Synthesis of new bis(triethylphosphine)platinum(II) complexes containing heterocyclic selenones as potential inhibitors of human cancer: Experimental and theoretical investigations

ASAdam A. A. SulaimanKing Fahd University of Petroleum and Minerals GBGaurav BhatiaGovernment of Himachal Pradesh MFMohammed FettouhiKing Fahd University of Petroleum and Minerals

Key Points

This research aims to synthesize and characterize new platinum(II) complexes with selenone ligands to evaluate their potential as cancer inhibitors.
Synthesis of seven platinum(II) complexes using bis(triethylphosphine) and various selenones.
Characterization through elemental analysis, FTIR, NMR spectroscopy, and single crystal X-ray diffraction.
In vitro cytotoxicity testing against HeLa, HCT-15, and MG-63 cancer cell lines and molecular docking studies with target DNA.
Complexes 3 and 4 showed higher cytotoxic efficacy compared to cisplatin against cancer cell lines.
All synthesized complexes exhibited stronger binding affinity to DNA than cisplatin during docking studies.
Complex 4 met the ADME-Tox criteria indicating favorable drug-like properties.

Abstract

Today, there is a significant demand for a new generation category of metal-based medicines capable of minimizing side effects while simultaneously improving efficacy against cancers that have acquired resistance to cisplatin. Seven new complexes of platinum(II) (1-7) derived from bis(triethylphosphine) and selenone ligands with the general the formulas Pt(Et 3 P) 2 (Selenone) 2 Cl 2 for complexes (1, 2, and 7), and Pt(Et 3 P) 2 (Selenone) 2 (PF 6 ) 2 for complexes (3-6) have been synthesized. Where formulas of selenones are (1,3-Imidazolidine-2-selenone (ImSe); N-methyl-1,3-Imidazolidine-2-selenone (MeImSe); N-ethyl-1,3-Imidazolidine-2-selenone (EtImSe), N-i-propyl-1,3-Imidazolidine-2-selenone (i-prImSe); 1,3-Diazinane-2-selenone (DiazSe); 1,3-Diazepane-2-selenone (DiapSe)). These complexes were comprehensively characterized by elemental analysis, fourier-transform infrared (FTIR) spectroscopy, and nuclear magnetic resonance (NMR) spectroscopy, including 1 H, 13 C, 31 P, and 77 Se nuclei, which confirmed their structural composition. The crystal structures of complexes 3 and 5 were further elucidated using single crystal X-ray diffraction, which revealed a deformed square planar arrangement around the platinum center due to the coordination of selenone and platinum(II) ion. This configuration aligns with the expected geometry for platinum(II) complexes, enhancing stability and potential reactivity.The cytotoxic effects of the synthesized complexes, alongside cisplatin as a control, were evaluated in vitro against three human cancer cell lines: HeLa (cervical cancer), HCT-15 (colon adenocarcinoma), and MG-63 (osteosarcoma). Results from IC 50 calculations showed that these complexes exhibited cytotoxic effects ranging from promising to moderate. Notably, complexes 3 and 4 demonstrated higher efficacy compared to cisplatin, suggesting their potential as more effective anti-cancer agents. Molecular docking studies further investigated this potential, as all complexes displayed stronger binding affinity and lower inhibition constants within the target DNA binding pocket than cisplatin, indicating a superior docking profile. ADME-Tox predictions were conducted to assess drug-likeness and pharmacokinetic properties, revealing that complex 4 met all criteria of the Lipinski and Egan rules without violations. This favorable ADME-Tox profile highlighted complex 4 as a promising candidate for drug development.

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