In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety

Publication date: Available online 14 February 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Isabella Rimoldi, Giorgio Facchetti, Giorgio Lucchini, Elisa Castiglioni, Silvia Marchianò, Nicola Ferri
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.

Graphical abstract

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