Design, Syntheses and Anticancer Activities of Platinum(IV) Prodrugs with Dihydrogen Phosphate as an Axial Ligand

被引:2
|
作者
Gao An-Li [1 ]
Xiong Qing-Feng [1 ]
Jiang Jing [1 ]
Yu Juan [1 ]
Lou Li-Guang [2 ]
Liu Wei-Ping [1 ]
机构
[1] Kunming Inst Precious Met, Platinum Based Drug Lab, Kunming 650106, Yunnan, Peoples R China
[2] Chinese Acad Sci, Shanghai Inst Mat Med, Tumor Pharmacol Lab, Shanghai 201203, Peoples R China
关键词
platinum(IV) complexes; synthesis; characterization; anticancer activity; COMPLEXES; DELIVERY; REDUCTION; AGENTS;
D O I
10.11862/CJIC.2018.211
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
CPL-1501 and CPL-1504, two platinum(IV) prodrugs with dihydrogen phosphate as one axial ligand, were synthesized from cisplatin and oxaliplatin, respectively, as the starting material, and characterized by elemental analysis, IR as well as C-13 and P-31 NMR. Their reduction potential was measured via the cyclic voltammetry. The standard MTT was used to evaluate anticancer activity of the two prodrugs against several human cancer cell lines. CPL-1501 has a good water-solubility (10 mg.mL(-1)) and water-stability. With the favorable E-p values, it can be readily reduced to an active prototype cisplatin in the oxygen-deprived micro-environment of cancer cells. The biological tests reveal that CPL-1501 is able to inhibit the growth of cancer cells and its anticancer activity is comparable to that of cisplatin but much greater than that of carboplatin, whereas CPL-1504 does not show significant activity, probably due to its lower E-p values.
引用
收藏
页码:1649 / 1654
页数:6
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