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| Home > Articles > Published articles > Synthesis and In Vitro Studies of Photoactivatable Semisquaraine-type Pt(II) Complexes |
(Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) (University of Granada. Departamento de Química Inorgánica) (Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Química) (Universitat Autònoma de Barcelona. Departament de Química)
| Date: | 2022 |
| Abstract: | The synthesis, full characterization, photochemical properties, and cytotoxic activity toward cisplatin-resistant cancer cell lines of new semisquaraine-type Pt(II) complexes are presented. The synthesis of eight semisquaraine-type ligands has been carried out by means of an innovative, straightforward methodology. A thorough structural NMR and X-ray diffraction analysis of the new ligands and complexes has been done. Density functional theory calculations have allowed to assign the trans configuration of the platinum center. Through the structural modification of the ligands, it has been possible to synthesize some complexes, which have turned out to be photoactive at wavelengths that allow their activation in cell cultures and, importantly, two of them show remarkable solubility in biological media. Photodegradation processes have been studied in depth, including the structural identification of photoproducts, thus justifying the changes observed after irradiation. From biological assessment, complexes C7 and C8 have been demonstrated to behave as promising photoactivatable compounds in the assayed cancer cell lines. Upon photoactivation, both complexes are capable of inducing a higher cytotoxic effect on the tested cells compared with nonphotoactivated compounds. Among the observed results, it is remarkable to note that C7 showed a PI > 50 in HeLa cells, and C8 showed a PI > 40 in A2780 cells, being also effective over cisplatin-resistant A2780cis cells (PI = 7 and PI = 4, respectively). The mechanism of action of these complexes has been studied, revealing that these photoactivated platinum complexes would actually present a combined mode of action, a therapeutically potential advantage. The synthesis, full characterization, photochemical properties, and cytotoxic activity toward cisplatin-resistant cancer cell lines of new semisquaraine-type Pt(II) complexes are presented. Eight semisquaraine-type ligands and their corresponding Pt(II) complexes have been studied. These complexes have turned out to be photoactive at wavelengths that allow their activation in cell cultures. Two of them display remarkable solubility in biological media showing a promising behavior as photoactivatable compounds against several cancer cell lines. |
| Grants: | Ministerio de Economía y Competitividad BIO2015-67358-C2-2-P Ministerio de Ciencia e Innovación CTQ2016-75363-R Agència de Gestió d'Ajuts Universitaris i de Recerca 2017/SGR-864 Agencia Estatal de Investigación RTI2018-098027-B-C22 |
| Note: | Altres ajuts: acords transformatius de la UAB |
| Rights: | Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original.  |
| Language: | Anglès |
| Document: | Article ; recerca ; Versió publicada |
| Published in: | Inorganic chemistry, Vol. 61, Issue 20 (May 2022) , p. 7729-7745, ISSN 1520-510X |
