Design, synthesis and biological evaluation of a novel platinum(Ⅱ)complex possessing bioreductive groups for cancer therapy

被引：0

作者：

Chengken Chen ^{[1
,2
]}

Chunmei Gao ^{[3
]}

Zigao Yuan ^{[2
,4
]}

Yuyang Jiang ^{[2
,5
,4
]}

机构：

[1] Department of Chemistry, Tsinghua University

[2] The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, The Graduate School at Shenzhen, Tsinghua University

[3] College of Chemistry and Chemical Engineering, Shenzhen University

[4] Shenzhen Kivita Innovative Drug Discovery Institute

[5] Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University

来源：

ChineseChemicalLetters | 2019年 / 30卷 / 01期

关键词：

Platinum compounds; Bioreductive; Nitrophenylalkanoic group; Cellular uptake; Antitumor;

D O I：

暂无

中图分类号：

O641.4 [络合物化学（配位化学）]; TQ460.1 [基础理论];

学科分类号：

070304 ; 081704 ; 1007 ;

摘要：

Cisplatin is one of the most successful antitumor agents, yet also restricted by its poor cellular uptake and low selectivity. Since 3-(2-nitrophenyl) propionic acid(NPPA) has been reported as a bioreductive prodrug moiety, herein we combined NPPA with cisplatin(compound 1) to improve its lipophilicity and targetability and then to improve the antitumor outcomes. In addition, compound 2 possessing 3-phenyl propionic acid(PPA) was also synthesized as a comparison to test the influence of the NPPA to the cytotoxicity, since PPA was not a bioreductive moiety. Bioevaluations showed that 1 displayed more potent antitumor potency than cisplatin and 2, suggesting Pt(II) complexes possessing NPPA groups may be a good strategy for future platinum drug discovery.

引用

页码：243 / 246

页数：4