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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and biological evaluation of naphthalenebenzimidizole platinum (II) complexes as potential antitumor agents
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Design, synthesis and biological evaluation of naphthalenebenzimidizole platinum (II) complexes as potential antitumor agents

机译：萘异戊酰胺铂（II）复合物作为潜在抗肿瘤剂的设计，合成及生物学评价

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摘要

A serial of naphthalenebenzimidizole-Pt complexes 1-6 were designed and synthesized as antitumor agents. In vitro antitumor assay results showed that complexes 1-6 exhibited moderate to high anti-proliferative activity against Hela, HepG2, SKOV-3, NCl-H460, BEL-7404 and A549 cancer cell lines, while they displayed obvious sensitivity and selectivity against SMMC-7721 and U251 cell lines and low toxicity against normal HL-7702 cells, in comparison with cisplatin. In vivo antitumor assay results indicated that complex 1 and 5 exhibited important in vivo antiproliferative activity in the NCI-460 and SMMC-7721 models, in comparison with cisplatin, respectively. Complexes 1 and 5 exhibited better antiproliferative activity against A549CDDP and SKOV3CDDP cell lines than cisplatin, with IC50 values of 6.98 +/- 0.47 mu M, 5.62 +/- 0.88 mu M and 13.13 +/- 2.11 mu M, 5.30 +/- 0.33 mu M, respectively, while they displayed potential antiproliferation against A549 and SKOV3 cell lines, with IC50 values of 7.32 +/- 0.51 mu M, 5.19 +/- 0.49 mu M and 14.92 +/- 0.11 mu M, 12.19 +/- 0.92 mu M, indicating the introduction of naphthalenebenzimidizole into platinum-metal system may overcome the resistance. Mechanistic studies showed that the representative complexes 1 and 5 exerted the antitumor effect mainly by the obvious covalent binding with DNA and the upregulation of the expression level of intracellular topo I, showing different action mechanism from cisplatin. (C) 2020 Elsevier Masson SAS. All rights reserved.
机译：设计并合成萘甲苯氨苄酰胺-PT复合物1-6作为抗肿瘤剂。体外抗肿瘤测定结果表明，复合物1-6对Hela，Hepg2，Skov-3，Ncl-H460，Bel-7404和A549癌细胞系的高度至高抗增殖活性表现出中度至高抗增殖活性，同时它们对SMMC表示了明显的敏感性和选择性与顺铂相比，-7721和U251细胞系对对正常HL-7702细胞的低毒性。在体内抗肿瘤测定中，结果表明，与顺铂分别相比，络合物1和5在NCI-460和SMMC-7721模型中表现出在体内抗增殖活性。复合物1和5对A549CDDP和SKOV3CDDP细胞系具有比顺铂的更好的抗增殖活性，IC50值为6.98 +/- 0.47 mu m，5.62 +/- 0.88 mu m和13.13 +/- 2.11 mu m，5.30 +/- 0.33分别为莫米，同时它们展示针对A549和SKOV3细胞系的潜在抗溶解，IC50值为7.32 +/-0.51μm，5.19 +/- 0.49 mu m和14.92 +/- 0.11 mu m，12.19 +/- 0.92 MU M，表明将萘苯并酰胺的引入铂金属系统可以克服抗性。机械研究表明，代表性复合物1和5主要通过与DNA的明显共价结合和细胞内Topo I的表达水平的上调，显示来自顺铂的不同作用机制的抗肿瘤效应。 （c）2020 Elsevier Masson SAS。版权所有。

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