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Current Developments in Pt(IV) Prodrugs Conjugated with Bioactive Ligands.
Bioinorganic Chemistry and Applications ( IF 4.7 ) Pub Date : 2018-10-01 , DOI: 10.1155/2018/8276139
Xuejiao Li 1 , Yahong Liu 2 , Hongqi Tian 1
Affiliation  

To overcome the side effects of and resistance to cisplatin, a variety of Pt(IV) prodrugs were designed and synthesized via different modifications including combination with lipid chains to increase hydrophobicity, conjugation with short peptide chains or nanoparticles to improve drug delivery, or addition of bioactive ligands to the axial positions of Pt(IV) complexes to exert dual-function effects. This review summarizes the recent progress in the development of Pt(IV) prodrugs conjugated with bioactive-targeting ligands, including histone deacetylase inhibitors, p53 agonists, alkylating agents, and nonsteroidal anti-inflammatory agents. Although Pt(IV) complexes that conjugated with bioactive ligands show satisfactory anticancer effects, none has been approved for clinical use. Therefore, we hope that this review will contribute to further study and development of Pt(IV) complexes conjugated with bioactive and other ligands.

中文翻译:


与生物活性配体缀合的 Pt(IV) 前药的最新进展。



为了克服顺铂的副作用和耐药性,通过不同的修饰设计和合成了多种 Pt(IV) 前药,包括与脂质链组合以增加疏水性、与短肽链或纳米颗粒缀合以改善药物递送,或添加将生物活性配体连接到 Pt(IV) 配合物的轴向位置,以发挥双功能作用。本综述总结了与生物活性靶向配体缀合的 Pt(IV) 前药的最新进展,包括组蛋白脱乙酰酶抑制剂、p53 激动剂、烷化剂和非甾体抗炎药。尽管与生物活性配体缀合的 Pt(IV) 配合物显示出令人满意的抗癌效果,但尚未批准用于临床。因此,我们希望这篇综述将有助于进一步研究和开发与生物活性和其他配体缀合的 Pt(IV) 配合物。
更新日期:2018-10-01
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