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. Facchetti
Secondo
;
G. Lucchini;E. Castiglioni;S. Marchianò
Penultimo
;
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.
triple negative breast cancer; cationic platinum complex; imidazole; p53 expression; cell cycle
Settore CHIM/03 - Chimica Generale e Inorganica
Settore BIO/14 - Farmacologia
2017
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/491233
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