Preparation of Rhodium(III) complexes with 2(1H)-quinolinone derivatives and evaluation of their in vitro and in vivo antitumor activity
Preparation of Rhodium(III) complexes with 2(1H)-quinolinone derivatives and evaluation of their in vitro and in vivo antitumor activity
复制标题
2(1H)-喹啉酮衍生物铑(III)配合物的制备及其体内外抗肿瘤活性评价
DOI：
10.1016/j.ejmech.2018.03.074
复制
发表时间：
2018
影响因子：
6.7
通讯作者：
Peng Yan
中科院分区：
文献类型：
--
作者：
Lu Xing;Wu Yi-Ming;Yang Jing-Mei;Ma Feng-E.;Li Liang-Ping;Chen Sheng;Zhang Ye;Ni Qing-Ling;Pan Ying-Ming;Hong Xue;Peng Yan
A series of 2(1H)-quinolinone derivatives and their rhodium (III) complexes were designed and synthesized. All the rhodium (III) complexes exhibited higherin vitrocytotoxicity for Hep G2, HeLa 229, MGC80-3, and NCI-H460 human tumor cell lines than their ligands and cisplatin, and among them complex9was found to be selectively cytotoxic to tumor cells. Further investigation revealed that complex9caused cell cycle arrest at the G2/M phase and induced apoptosis, and inhibited the proliferation of Hep G2 cells by impeding the phosphorylation of epidermal growth factor receptor (EGFR) and its downstream enzymes. Complex9also up-regulated the proapoptotic proteins Bak, Bax, and Bim, which altogether activated caspase-3/9 to initiate cell apoptosis. Notably, complex9effectively inhibited tumor growth in the NCI-H460 xenograft mouse model with less adverse effect than cisplatin.
