Premium
Biphosphine Palladium(II) and Platinum(II) Complexes: Synthesis, Docking, and Cytotoxicity
Author(s) -
AbuSurrah Adnan S.,
Sunjuk Mahmoud,
Tahtamouni Lubna,
AlNajjar Lana,
Ayyad Jumana,
AlSharaa Wiam,
Shtaiwi Amneh
Publication year - 2025
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202500894
Abstract Palladium(II) ( 1A – 4A ) and platinum(II) ( 1B , 2B, and 4B ) complexes bearing biphosphine ligands with different backbones and variable substituents on the phosphine donor atoms were prepared and characterized. Molecular docking of the complexes was performed. In silico analysis was performed to predict the “drug‐likeness” and ADMET properties. The in vitro cytotoxicity of these complexes against colorectal (HCT‐116), hepatocellular (HepG2), and breast (MCF‐7) cancer cells was also evaluated. The docking results demonstrated that all complexes exhibit good binding affinity to B‐DNA. Some of the Pd(II) complexes showed acceptable cytotoxic effects compared to cisplatin. Overall, the neutral palladium(II) complexes with the selected biphosphine ligands displayed better cytotoxicity than their corresponding Pt(II) analogues. Among them, the Pd(II) complex 4A , bearing the biphosphine ligand with bulky aliphatic axial substituents and a reduced bite angle, showed the highest DNA‐binding affinity and excellent cytotoxic activity (IC 50 = 14.2 µM against the MCF‐7 cancer cell line) compared to cisplatin (IC 50 = 31.3 µM) and the corresponding Pt(II) complex 4B (IC 50 = 132.9 µM). In addition, complex 4A demonstrated exceptional antitumor selectivity (selectivity index value of 9.5) as compared to that of cisplatin (SI = 1.3). Since the electronic, structural, and chiral properties of these ligands can be easily turned, Pd(II) complexes with large aliphatic axial substituents biphosphine ligands (such as complex 4A ) may represent a promising alternative for cancer treatment.
Accelerating Research
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom
Address
John Eccles HouseRobert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom