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

[Display omitted] 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...

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Published in:Bioorganic & medicinal chemistry 2017-03, Vol.25 (6), p.1907-1913
Main Authors: Rimoldi, Isabella, Facchetti, Giorgio, Lucchini, Giorgio, Castiglioni, Elisa, Marchianò, Silvia, Ferri, Nicola
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cationic platinum complex
Cell cycle
Cell Division - drug effects
Cell Line, Tumor
Chromatography, High Pressure Liquid
Chromatography, Reverse-Phase
Drug Evaluation, Preclinical
Humans
Imidazole
Imidazoles - chemistry
Organoplatinum Compounds - chemistry
Organoplatinum Compounds - pharmacology
p53 expression
Triple negative breast cancer
Triple Negative Breast Neoplasms - pathology
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Summary:[Display omitted] 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=61.9µM) and more effective than cisplatin on both DLD-1 (IC50=57.4µM) and MCF-7 (IC50=79.9µM) 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2017.02.010