Preparation and Biological Evaluation of Two Novel Platinum(II) Complexes Based on the Ligands of Dipicolyamine Bisphosphonate Esters

被引：9

作者：

Qiu, Ling ^{[1
]}

Liu, Hong ^{[1
]}

Li, Ke ^{[1
]}

Lv, Gaochao ^{[1
]}

Yang, Hui ^{[1
]}

Qin, Xiaofeng ^{[1
]}

Lin, Jianguo ^{[1
]}

机构：

[1] Minist Hlth, Jiangsu Key Lab Mol Nucl Med, Key Lab Nucl Med, Jiangsu Inst Nucl Med, Wuxi 214063, Peoples R China

来源：

MOLECULES | 2016年 / 21卷 / 03期

基金：

中国国家自然科学基金;

关键词：

dipicolyamine bisphosphonate ester; platinum complex; hydroxyapatite affinity; antitumor activity; action mechanism; IN-VITRO; DNA; CYTOTOXICITY; DELIVERY;

D O I：

10.3390/molecules21030255

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Two new platinum(II)-based complexes bearing a bone-targeting group were synthesized and characterized. They both have excellent affinity for hydroxyapatite (HA), which is abundant in human bone tissues. Their antitumor activities against five human cancer cell lines (U2OS, A549, HCT116, MDA-MB-231 and HepG2) were evaluated and compared with cisplatin (CDDP). Though the antitumor efficacies of new complexes are lower than that of CDDP, they show higher selectivity against the HepG2 hepatoma cell line than the L02 normal liver cell line. Morphology studies exhibited typical characteristics of cell apoptosis and the cell cycle distribution analysis indicated that the complexes can inhibit cancer cells by inducing cell cycle arrest at the G2/M phase, a similar mechanism of action to CDDP.

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页数：13

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