Preliminary Study of the Cytotoxic Activity of Pd(II) and Pt(II) Complexes Bearing P-N ligands Derived from Aminoalcohols

Iminophosphine ligands find extensive applications in homogeneous catalysis; however, their potential antitumor activity is currently being explored. Including biologically active moieties, such as aminoalcohols, could enhance this activity further. Therefore, we have synthesised a novel series of Pd(II) and Pt(II) iminophosphine complexes incorporating aminoalcohols as biologically active moieties to explore the potential of enhancing this activity. The series of Pd(II) complexes includes complexes 2a, 2f, and 2h, which were previously reported by our research group as catalysts in Suzuki–Miyaura cross-coupling reaction in aqueous media. Besides their complete characterisation, some structures have been unequivocally corroborated by single-crystal X-ray diffraction (SC-XRD). To evaluate the cytotoxic potential of the complexes, a preliminary in vitro study was conducted on different cancerous cell lines, including using COS-7 cells as a healthy cell line. Notably, complexes 2e, 2f, and 3b exhibited selectivity towards human chronic myelogenous leukaemia (K562), demonstrating IC50 values of 7.73 ± 1.4 µM, 8.53 ± 1.9 µM, and 8.83 ± 1.5 µM, respectively. Remarkably, the selectivity of these complexes surpassed that of cisplatin. Furthermore, in silico analysis indicated a higher binding energy of these complexes to DNA when compared to cisplatin.

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Journal
Inorganics
Published
2025-12-02
DOI
https://doi.org/10.3390/inorganics13120398
Primary Topic
Catalytic Cross-Coupling Reactions
Type
article
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article

Preliminary Study of the Cytotoxic Activity of Pd(II) and Pt(II) Complexes Bearing P-N ligands Derived from Aminoalcohols

Juan S. Serrano‐García, Viviana Reyes‐Márquez, Jorge Alí‐Torres, David Morales‐Morales et al.
Inorganics
Catalytic Cross-Coupling Reactions
article

Preliminary Study of the Cytotoxic Activity of Pd(II) and Pt(II) Complexes Bearing P-N ligands Derived from Aminoalcohols

Juan S. Serrano‐García, Viviana Reyes‐Márquez, Jorge Alí‐Torres, David Morales‐Morales, Jair Isai Ortega-Gaxiola, Simón Hernández‐Ortega, Raúl Colorado‐Peralta, Antonino Arenaza‐Corona, Adrián L. Orjuela, Andrés Amaya‐Flórez, Jordi R.‐Galindo, Teresa Ramírez‐Ápan, Michelle Acosta-Encinas
article en

Abstract

Iminophosphine ligands find extensive applications in homogeneous catalysis; however, their potential antitumor activity is currently being explored. Including biologically active moieties, such as aminoalcohols, could enhance this activity further. Therefore, we have synthesised a novel series of Pd(II) and Pt(II) iminophosphine complexes incorporating aminoalcohols as biologically active moieties to explore the potential of enhancing this activity. The series of Pd(II) complexes includes complexes 2a, 2f, and 2h, which were previously reported by our research group as catalysts in Suzuki–Miyaura cross-coupling reaction in aqueous media. Besides their complete characterisation, some structures have been unequivocally corroborated by single-crystal X-ray diffraction (SC-XRD). To evaluate the cytotoxic potential of the complexes, a preliminary in vitro study was conducted on different cancerous cell lines, including using COS-7 cells as a healthy cell line. Notably, complexes 2e, 2f, and 3b exhibited selectivity towards human chronic myelogenous leukaemia (K562), demonstrating IC50 values of 7.73 ± 1.4 µM, 8.53 ± 1.9 µM, and 8.83 ± 1.5 µM, respectively. Remarkably, the selectivity of these complexes surpassed that of cisplatin. Furthermore, in silico analysis indicated a higher binding energy of these complexes to DNA when compared to cisplatin.

InorganicsVol. 13(12)
Universidad Veracruzana (MX), Universidad Nacional de Colombia (CO), Universidad de Sonora (MX), Instituto de Investigaciones Científicas y Servicios de Alta Tecnología (PA), Universidad Nacional Autónoma de México (MX)
Dirección General de Asuntos del Personal Académico, Universidad Nacional Autónoma de México
Openalex Percentile: Top 71%
Catalytic Cross-Coupling Reactions
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