Preparation and Biological Evaluation of Two Novel Platinum(II) Complexes Based on the Ligands of Dipicolyamine Bisphosphonate Esters.
Preparation and Biological Evaluation of Two Novel Platinum(II) Complexes Based on the Ligands of Dipicolyamine Bisphosphonate Esters.
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两种基于二吡啶二胺双膦酸酯配体的新型铂(II)配合物的制备及生物学评价
DOI：
10.3390/molecules21030255
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发表时间：
2016-02-24
期刊：
影响因子：
--
通讯作者：
Lin J
中科院分区：
文献类型：
--
作者：
Qiu L;Liu H;Li K;Lv G;Yang H;Qin X;Lin J
合成了两种新的具有骨靶向基团的铂（II）基配合物，并进行了表征。它们都对人体骨组织中丰富的羟基磷灰石（HA）具有良好的亲和力。对5种人癌细胞株（U2 OS、A549、HCT 116、MDA-MB-231和HepG 2）进行体外抗肿瘤活性测定，并与顺铂（CDDP）进行比较。虽然新配合物的抗肿瘤效力低于CDDP，但它们对HepG 2肝癌细胞系的选择性高于L02正常肝细胞系。形态学研究显示了典型的细胞凋亡特征，细胞周期分布分析表明，配合物可以通过诱导细胞周期停滞在G2/M期来抑制癌细胞，这与CDDP的作用机制相似。
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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影响因子：
19
作者：
Palazzo, Barbara;Iafisco, Michele;Roveri, Norberto
通讯作者：
Roveri, Norberto
DOI：
10.1016/j.jchromb.2009.08.007
发表时间：
2009-10-01
影响因子：
3
作者：
Tarcomnicu, Isabela;Gheorghe, Mihaela Cristina;Tudoroniu, Ariana
通讯作者：
Tudoroniu, Ariana
DOI：
10.1039/b908652h
发表时间：
2009-08-28
期刊：
Chemical communications (Cambridge, England)
影响因子：
--
作者：
Torres Martin de Rosales R;Finucane C;Mather SJ;Blower PJ
通讯作者：
Blower PJ
影响因子：
2.9
作者：
WOLFE, A;SHIMER, GH;MEEHAN, T
通讯作者：
MEEHAN, T
影响因子：
5.1
作者：
Carotti, S;Marcon, G;Orioli, P
通讯作者：
Orioli, P