Mitochondria-Targeted Benzoxazole-Based Platinum Photosensitizer Complexes: Photophysical Properties and Photocytotoxicity Evaluation Against Breast and Gastric Cancer Cells.
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This study explores platinum(II) phototherapy using cycloplatinated compounds with bidentate 2-(4-substituted) benzoxazole ligands, [Pt()()()] ().
APA
Rabor JT, Mandegani Z, et al. (2025). Mitochondria-Targeted Benzoxazole-Based Platinum Photosensitizer Complexes: Photophysical Properties and Photocytotoxicity Evaluation Against Breast and Gastric Cancer Cells.. Journal of medicinal chemistry, 68(16), 17065-17086. https://doi.org/10.1021/acs.jmedchem.5c00543
MLA
Rabor JT, et al.. "Mitochondria-Targeted Benzoxazole-Based Platinum Photosensitizer Complexes: Photophysical Properties and Photocytotoxicity Evaluation Against Breast and Gastric Cancer Cells.." Journal of medicinal chemistry, vol. 68, no. 16, 2025, pp. 17065-17086.
PMID
40785274 ↗
Abstract 한글 요약
This study explores platinum(II) phototherapy using cycloplatinated compounds with bidentate 2-(4-substituted) benzoxazole ligands, [Pt()()()] (). The compounds were synthesized and fully characterized, and their photophysical, cytotoxic, and phototoxic properties were analyzed. Time-dependent Density Functional Theory (TD-DFT) calculations supported the analysis of the complexes absorption and photoluminescence, with high-energy absorption showing L'LCT/MLCT [π(Cl, Me) → π*(C^N)] contributions. Among the complexes, ( = C^N, = κ--C^N, = Cl) exhibited the highest quantum yield (Φ = 48%) and showed strong antiproliferative activity in breast carcinoma (MCF-7) and gastric adenocarcinoma (AGS) cell lines. (, = N^N, = Cl, = Cl, , = N^N, = Me, = Me; , = C^N, = DMSO, = Cl; , = C^N, = C^N, = Cl, and , = C^N, = Me, = DMSO) also demonstrated potential as photoactivatable agents. Mechanistic studies indicated that the complexes triggered ROS generation, mitochondrial dysfunction, and lysosomal damage, with showing promise for photochemotherapeutic treatment of gastric and breast cancer due to its selectivity and effectiveness in targeting mitochondria and lysosomes.
🏷️ 키워드 / MeSH 📖 같은 키워드 OA만
- Humans
- Photosensitizing Agents
- Mitochondria
- Benzoxazoles
- Stomach Neoplasms
- Antineoplastic Agents
- Breast Neoplasms
- Female
- Cell Line
- Tumor
- Density Functional Theory
- Structure-Activity Relationship
- Cell Proliferation
- Drug Screening Assays
- Antitumor
- Organoplatinum Compounds
- Reactive Oxygen Species
- MCF-7 Cells
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