Issue 24, 2013
From the journal:

Chemical Communications

Highly water-soluble platinum(ii) complexes as GLUT substrates for targeted therapy: improved anticancer efficacy and transporter-mediated cytotoxic properties†

Pengxing Liu,a   Yanhui Lu,a   Xiangqian Gao,a   Ran Liu,a   Daisy Zhang-Negrerie,a   Ying Shi,b   Yiqiang Wang,c   Songqing Wanga  and  Qingzhi Gao*a  

* Corresponding authors

a Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Nankai District, Tianjin 300072, P. R. China
E-mail: qingzhi@gmail.com
Fax: +86 22 2789-2050
Tel: +86135 1247-9137

b Central Institute of Pharmaceutical Research, CSPC Pharmaceutical Group, 226 Huanhe Road, Shijiazhuang, Hebei 050035, P. R. China

c Department of Medicinal Chemistry, Gudui BioPharma Technology Inc., 2 Huatian Road, Huayuan Industrial Park, Tianjin 300384, P. R. China

Abstract

Glucose-conjugated malonato-platinum(II) complexes are designed and synthesized to target tumor-specific active transporters, namely, glucose transporters (GLUTs); the complexes exhibit much higher aqueous solubility by 150 times, improved potency in cytotoxicities by 10 times, and increased therapeutic index by over 30 fold compared to the newest generation of clinical drugs oxaliplatin.

Graphical abstract: Highly water-soluble platinum(ii) complexes as GLUT substrates for targeted therapy: improved anticancer efficacy and transporter-mediated cytotoxic properties

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Article information

DOI
https://doi.org/10.1039/C3CC38589B
Article type
Communication
Submitted
29 Nov 2012
Accepted
01 Feb 2013
First published
01 Feb 2013

Chem. Commun., 2013,49, 2421-2423

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Highly water-soluble platinum(II) complexes as GLUT substrates for targeted therapy: improved anticancer efficacy and transporter-mediated cytotoxic properties

P. Liu, Y. Lu, X. Gao, R. Liu, D. Zhang-Negrerie, Y. Shi, Y. Wang, S. Wang and Q. Gao, Chem. Commun., 2013, 49, 2421 DOI: 10.1039/C3CC38589B

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