| Institution: | 1. MAT-InLAB, LASCAMM CR-INSTM, Unità INSTM della Calabria, Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Ponte Pietro Bucci Cubo 14C, 87036 Arcavacata di Rende (CS), Italy;2. MAT-InLAB, LASCAMM CR-INSTM, Unità INSTM della Calabria, Dipartimento di Chimica e Tecnologie Chimiche, Università della Calabria, Ponte Pietro Bucci Cubo 14C, 87036 Arcavacata di Rende (CS), Italy
CNR NANOTEC-Istituto di Nanotecnologia UOS Cosenza, 87036 Arcavacata di Rende (CS), Italy;3. CNR NANOTEC-Istituto di Nanotecnologia UOS Cosenza, 87036 Arcavacata di Rende (CS), Italy;4. Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, Via Marzolo 5, 35131 Padua, Italy;5. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Venezian 21, 20133 Milan, Italy |
| Abstract: | The in vitro biological activity towards the MDA-MB-231 triple-negative breast cancer cell line of two different series of anionic Pt(II) organometallic complexes was tested. For the first time, cytotoxic activity of anionic Pt(II) complexes has been observed. The anionic compounds of general formula NBu4(C^N)Pt(O^O)], where (C^N) represents the cyclometalated form of 2-phenylpyridine (H(PhPy)), 2-thienylpyridine (H(Thpy)) or 2-benzoh]quinoline (H(Bzq)), feature two different (O^O) chelated ligands: tetrabromocatechol BrCat]2? ( 1 – 3 ) or alizarine Aliz]2? ( 4 – 6 ). Complexes 1 – 6 displayed a significant cytotoxic effect against the studied cell line (IC50 range of 1.9–52.8 μM). For BrCat-containing complexes 1 – 3 , the biological activity was independent of the nature of the coordinated (C^N) ligand. In contrast, in the case of 4 – 6 , the cytotoxicity (significantly high for 4 ) was concomitantly induced by the presence of either the PhPy or the Aliz]2? ligand. Since complexes 1–6 are emissive in solution, the potential use of 4 as a theranostic agent was investigated using confocal analysis. The fluorescence signal from MDA-MB-231 cells incubated with 4 indicated the localization of the compound into the cytosol region. |
