Synthesis and In Vitro Studies of Photoactivatable Semisquaraine-type Pt(II) Complexes

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The synthesis, full characterization, photochemical properties, and cytotoxic activity towards cisplatin-resistant cancer cell lines of new semisquaraine-type Pt(II) complexes is presented. The synthesis of eight semisquaraino-type ligands has been carried out by means of an innovative, straightforward methodology. A thorough structural NMR and XRD analysis of the new ligands and complexes has been done. DFT calculations have allowed to establish 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 deep, 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 higher cytotoxic effect on the tested cells compared with non-photoactivated 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 photo-activated platinum complexes would actually present a combined mode of action, a therapeutically potential advantage.
Original languageEnglish
JournalInorganic Chemistry
Publication statusAccepted in press - 2022


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