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Molecules 2016, 21(3), 255; doi:10.3390/molecules21030255

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

Jiangsu Key Laboratory of Molecular Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
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Academic Editors: Jean Jacques Vanden Eynde and Annie Mayence
Received: 30 December 2015 / Revised: 1 February 2016 / Accepted: 2 February 2016 / Published: 24 February 2016
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Abstract

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. View Full-Text
Keywords: dipicolyamine bisphosphonate ester; platinum complex; hydroxyapatite affinity; antitumor activity; action mechanism dipicolyamine bisphosphonate ester; platinum complex; hydroxyapatite affinity; antitumor activity; action mechanism
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Qiu, L.; Liu, H.; Li, K.; Lv, G.; Yang, H.; Qin, X.; Lin, J. Preparation and Biological Evaluation of Two Novel Platinum(II) Complexes Based on the Ligands of Dipicolyamine Bisphosphonate Esters. Molecules 2016, 21, 255.

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