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http://hdl.handle.net/10662/13564
Títulos: | Influence of ligand lipophilicity in Pt(II) complexes on their antiproliferative and apoptotic activities in tumour cell lines |
Autores/as: | Fernández Delgado, Elena Estirado Rivera, Samuel Espino Palma, Javier Viñuelas Zahínos, Emilio Luna Giles, Francisco Rodríguez Moratinos, Ana Beatriz Pariente Llanos, José Antonio |
Palabras clave: | N,S-heterocycles;Lipophilicity;Cytotoxicity;Apoptosis;Pt(II) complexes;Chemotherapeutics in tumour cells;Citotoxicidad;Complejos de Pt(II);Quimioterapéuticos en células tumorales;N,S-heterociclos;Lipofilicidad |
Fecha de publicación: | 2021 |
Editor/a: | Elsevier |
Resumen: | One of the most widely used strategies for drug development is the coordination of bioactive ligands to transition metals, which could improve biological activity. Moreover, the incorporation of aromatic groups to ligands may allow an enhanced lipophilicity that can influence the cellular uptake and accumulation of the metallodrugs, thus increasing their activity. Herein, we have reported the synthesis and characterization of four Pt(II) complexes [PtCl2(L)], where L = 2-(1-pyrazolyl)-2-thiazoline (PzTn), 2-(1-pyrazolyl)-1,3-thiazine (PzTz), 2-(3,5-diphenyl-1- pyrazolyl)-2-thiazoline (DPhPzTn) or 2-(3,5-diphenyl-1-pyrazolyl)-1,3-thiazine (DPhPzTz). The study was aimed at analysing their potential anticarcinogenic ability in epithelial cervix carcinoma HeLa, human promyelocytic leukemia HL-60 and human histiocytic lymphoma U-937 tumour cell lines as well as checking whether the structural factors of the organic ligand may influence their biological activity. Our findings showed that PtDPhPzTn and PtDPhPzTz were far more effective in terms of cytotoxicity than their less lipophilic counterparts (PtPzTn and PtPzTz), especially in cells derived from solid cervical tumours, thereby suggesting that modulating the lipophilicity of the ligands can help improve the cytotoxic effect of the metal complexes. |
Descripción: | This manuscript is in Memoriam of Prof. Álvaro Bernalte García, Group Leader of the Coordination Chemistry Research Group. |
URI: | http://hdl.handle.net/10662/13564 |
DOI: | 10.1016/j.jinorgbio.2021.111688 |
Colección: | DFSIO - Artículos DQOIN - Artículos |
Archivos
Archivo | Descripción | Tamaño | Formato | |
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j.jinorgbio.2021.111688.pdf | 2,34 MB | Adobe PDF | Descargar |
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