Novel Pt(ii) complexes with modified aroyl-hydrazone Schiff-base ligands: synthesis, cytotoxicity and action mechanism
Novel Pt(ii) complexes with modified aroyl-hydrazone Schiff-base ligands: synthesis, cytotoxicity and action mechanism
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新型 Pt(ii) 与修饰芳酰腙席夫碱配体的配合物：合成、细胞毒性和作用机制
DOI：
10.1039/c9mt00193j
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发表时间：
2019
期刊：
影响因子：
3.4
通讯作者：
Yang Feng
中科院分区：
文献类型：
--
作者：
Deng Jungang;Yu Ping;Zhang Zhenlei;Zhang Juzheng;Zhewen Sun;Cai Meiling;Yuan Haoliang;Liang Hong;Yang Feng
To develop new anti-tumour Pt(ii) agents, we designed and synthesized five Pt(ii) complexes. These Pt(ii) complexes were modified benzene rings of 2-hydroxybenzylidene with a hydrocarbyl or halogen group. The five Pt(ii) complexes possessed remarkable cytotoxicity against tumour cellsin vitro. In particular, we investigated chemotherapeutic mechanisms of the complexes against A549cisR cells. The Pt(ii) complexes could bind to and cleave DNA, while also inducing arrest of the cell cycle in S phase, leading to down-regulation of the levels of cyclin-dependent kinases and cyclin and up-regulation of the expression of p21. The selected complex,C3, changed the mitochondrial membrane potential and induced apoptosis.C3also inhibited the expression of thec-mycgene and downstream proteins, thereby inhibiting telomerase activity.
