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

Rimoldi Isabella; Facchetti Giorgio; Lucchini GiorgioeCastiglioni ElisaMarchiano SilviaFerri Nicola

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

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

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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 mu M) and more effective than cisplatin on both DLD-1 (IC50 = 57.4 mu M) and MCF-7 (IC50= 79.9 mu M) 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. (C) 2017 Elsevier Ltd. All rights reserved.

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《Bioorganic and medicinal chemistry》 |2017年第6期|1907-1913|共7页
作者
Rimoldi Isabella; Facchetti Giorgio; Lucchini GiorgioeCastiglioni ElisaMarchiano SilviaFerri Nicola;
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作者单位

Univ Milan, Dipartimento Sci Agrarie Ambientali Produz, Via Balzaretti 9, I-20133 Milan, Italy;

Univ Milan, Dipartimento Sci Farmaceutiche, Via Venezian 21, I-20133 Milan, Italy;

Univ Padua, Dipartimento Sci Farmaco, Via Marzolo 5, I-35131 Padua, Italy;

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正文语种英语
中图分类药学;
关键词
Triple negative breast cancer; Cationic platinum complex; lmidazole; p53 expression; Cell cycle;

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

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