The development and the synthesis of cationic platinum(II) complexes were realized and their cytotoxic activity was tested on triple negative breast cancer MDA-MB-231 cell line and in two cell lines poorly responsive to cisplatin (DLD-1 and MCF-7). The complex 2c resulted the most potent cytotoxic agent in MDA-MB-231 (IC50=61.9 µM) and more effective than cisplatin on both DLD-1 (IC50=57.4 µM) and MCF-7 (IC50=79.9 µM) cell lines. 2c showed different cellular uptake and pharmacodynamic properties than cisplatin, interfering with the progression of the M phase of the cell cycle. Thus, 2c represents a lead compound of a new class of cytotoxic agents with promising antitumor activity.
In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety / I. Rimoldi, G. Facchetti, G. Lucchini, E. Castiglioni, S. Marchianò, N. Ferri. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 25:6(2017), pp. 1907-1913. [10.1016/j.bmc.2017.02.010]
In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety
I. Rimoldi
;G. FacchettiSecondo
;G. Lucchini;E. Castiglioni;S. MarchianòPenultimo
;
2017
Abstract
The development and the synthesis of cationic platinum(II) complexes were realized and their cytotoxic activity was tested on triple negative breast cancer MDA-MB-231 cell line and in two cell lines poorly responsive to cisplatin (DLD-1 and MCF-7). The complex 2c resulted the most potent cytotoxic agent in MDA-MB-231 (IC50=61.9 µM) and more effective than cisplatin on both DLD-1 (IC50=57.4 µM) and MCF-7 (IC50=79.9 µM) cell lines. 2c showed different cellular uptake and pharmacodynamic properties than cisplatin, interfering with the progression of the M phase of the cell cycle. Thus, 2c represents a lead compound of a new class of cytotoxic agents with promising antitumor activity.File | Dimensione | Formato | |
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