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<p>Cancer remains major health problem with a high mortality rate. Thiourea and its derivatives have been identified as potent agents for cancer treatment with thiourea complexes exhibiting high anticancer activity such as platinum complexes and palladium complexes. The objective of this study was to design and synthesize a novel palladium-based thiourea metal complex as an anticancer agent. In this study, novel N-((2-chloropyridin-3-yl)carbamothioyl)-3-yl)carbamothioyl)-3-methylbenzamide (L<sup>1</sup>) and N-((6-methylpyridin-2-yl) carbamothioyl)benzamide (L<sup>2</sup>) and their palladium (II) complexes ([PdL<sup>1</sup><sub>2</sub>] and [PdL<sup>2</sup><sub>2</sub>]) were synthesized. Structural characterization of all the synthesized compounds was conducted using FT-IR, ¹H-NMR, and 13&#xa0;C-NMR techniques. The anticancer properties of these palladium (II) complexes were subsequently investigated in colon cancer cell lines. To evaluate anti-tumor activity, the cytotoxic activities of the compounds were evaluated on CCD-18Co, SW620, and Caco-2 cells using a cell viability assay. The results demonstrated that the complexes were cytotoxic in a dose-dependent manner. Notably, [PdL<sup>2</sup><sub>2</sub>] exhibited cytotoxic effects at low concentrations in colon cancer cells. Next, cell cycle distribution and Annexin V assays were performed to determine the mechanism by which [PdL<sup>2</sup><sub>2</sub>] inhibits SW620 cell proliferation. In conclusion, [PdL<sup>2</sup><sub>2</sub>] preferentially induces cell death and cell cycle arrest in colon cancer cells via ROS production, displaying a favorable selectivity index (SI~ 6) relative to normal CCD-18Co fibroblasts.</p>

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Novel benzoylthioureas with pyridine and their Pd(II) complexes: preferentially inducing apoptosis via ROS in colon cancer cells

  • 期刊论文

  • 发表日期：

    2026年7月17日

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  • Muzaffer Dukel,
  • Fatih Mehmet Emen ,
  • Zümre Ayça Kalabalik,
  • Emine Kutlu ,
  • Muhammad Asim Ali

摘要

Cancer remains major health problem with a high mortality rate. Thiourea and its derivatives have been identified as potent agents for cancer treatment with thiourea complexes exhibiting high anticancer activity such as platinum complexes and palladium complexes. The objective of this study was to design and synthesize a novel palladium-based thiourea metal complex as an anticancer agent. In this study, novel N-((2-chloropyridin-3-yl)carbamothioyl)-3-yl)carbamothioyl)-3-methylbenzamide (L1) and N-((6-methylpyridin-2-yl) carbamothioyl)benzamide (L2) and their palladium (II) complexes ([PdL12] and [PdL22]) were synthesized. Structural characterization of all the synthesized compounds was conducted using FT-IR, ¹H-NMR, and 13 C-NMR techniques. The anticancer properties of these palladium (II) complexes were subsequently investigated in colon cancer cell lines. To evaluate anti-tumor activity, the cytotoxic activities of the compounds were evaluated on CCD-18Co, SW620, and Caco-2 cells using a cell viability assay. The results demonstrated that the complexes were cytotoxic in a dose-dependent manner. Notably, [PdL22] exhibited cytotoxic effects at low concentrations in colon cancer cells. Next, cell cycle distribution and Annexin V assays were performed to determine the mechanism by which [PdL22] inhibits SW620 cell proliferation. In conclusion, [PdL22] preferentially induces cell death and cell cycle arrest in colon cancer cells via ROS production, displaying a favorable selectivity index (SI~ 6) relative to normal CCD-18Co fibroblasts.