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oai:docta.ucm.es:20.500.14352/954992025-03-18T13:06:04Zcom_20.500.14352_14col_20.500.14352_15

00925njm 22002777a 4500 dc Durán Sampedro, Gonzalo author Xue, Evelyn . author Evelynoreno-Simoni, Evelyn author Paramio, Celia author Torres, Tomás author Ng, Dennis K. P. author Torre, Gema de la author 2023 Pt(II)-BODIPY complexes combine the chemotherapeutic activity of Pt(II) with the photocytotoxicity of BODIPYs. Additional conjugation with targeting ligands can boost the uptake by cancer cells that overexpress the corresponding receptors. We describe two Pt(II) triangles, 1 and 2, built with pyridyl BODIPYs functionalized with glucose (3) or triethylene glycol methyl ether (4), respectively. Both 1 and 2 showed higher singlet oxygen quantum yields than 3 and 4, due to the enhanced singlet-to -triplet intersystem crossing. To evaluate the targeting effect of the glycosylated derivative, in vitro experiments were performed using glucose transporter 1 (GLUT1)-positive HT29 and A549 cancer cells, and noncancerous HEK293 cells as control. Both 1 and 2 showed higher cellular uptake than 3 and 4. Specifically, 1 was selective and highly cytotoxic toward HT29 and A549 cells. The synergistic chemo-and photodynamic behavior of the metallacycles was also confirmed. Notably, 1 exhibited superior efficacy toward the cisplatin-resistant R-HepG2 cells. Enhance Cellular Uptake Chemotherapeutic Activity Photoeeneltlaen for PDT Durán-Sampedro, Gonzalo, et al. «Glycosylated BODIPY- Incorporated Pt(II) Metallacycles for Targeted and Synergistic Chemo-Photodynamic Therapy». Journal of Medicinal Chemistry, vol. 66, n.o 5, marzo de 2023, pp. 3448-59. https://doi.org/10.1021/acs.jmedchem.2c01940. 0022-2623 10.1021/acs.jmedchem.2c01940 https://hdl.handle.net/20.500.14352/95499 1520-4804 https://doi.org/10.1021/acs.jmedchem.2c01940 Glycosylated BODIPY- Incorporated Pt(II) Metallacycles for Targeted and Synergistic Chemo-Photodynamic Therapy