期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 17, 页码 7571-7582出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm300580y
关键词
-
资金
- Singapore Ministry of Education [R143-000-411-133, R143-000-512-112, R279-000-321-133]
- Singapore Ministry of Health's National Medical Research Council under the New Investigator Grant scheme
Platinum(II) anticancer drug cisplatin is one of the most important chemotherapeutic agents in clinical use but is limited by its high toxicity and severe side effects. Platinum(IV) anticancer prodrugs can overcome these limitations by resisting premature aquation and binding to essential plasma proteins. Structure activity relationship studies revealed a link between the efficacy of platinum(IV) complexes with the nature of their axial ligands, which can be modified to enhance the properties of the prodrug. The existing paradigm of employing platinum(IV) complexes with symmetrical axial carbox-ylate ligands does not fully exploit their vast potential. A new approach was conceived to control properties of platinum(IV) prodrugs using contrasting axial ligands via sequential acylation. We report a novel class of asymmetric platinum(IV) carboxylates based on the cisplatin template containing both hydrophilic and lipophilic ligands on the same scaffold designed to improve their aqueous properties and enhance their efficacy against cancer cells in vitro.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据