The Platin-X series: activation, targeting, and delivery.
The Platin-X series: activation, targeting, and delivery.
复制标题
DOI：
10.1039/c6dt01738j
复制
发表时间：
2016-08-16
期刊：
影响因子：
--
通讯作者：
Dhar S
中科院分区：
文献类型：
--
作者：
Basu U;Banik B;Wen R;Pathak RK;Dhar S
抗癌铂（Pt）配合物一直被认为是药物无机化学史上最大的成功案例之一。然而，人们仍在寻找能够满足有效化疗药物配方要求的“灵丹妙药”。Pt（IV）配合物在动力学上比Pt（II）同系物更具惰性，并提供附加额外官能团/配体的机会，用于前药激活，肿瘤靶向或药物递送。功能化的最终目的是增强肿瘤的选择性作用和减轻药物的全身毒性。此外，增加细胞积累以克服肿瘤对药物的耐药性在药物开发和发现中也是至关重要的。在这篇综述中，我们将讨论我们实验室开发的一些可以被激活的铂（IV）前药的尝试，以及它们使用强大的纳米技术平台的靶向递送。
Anticancer platinum (Pt) complexes have long been pronounced as one of the biggest success stories in the history of medicinal inorganic chemistry. Yet there still remains the hunt for the “magic bullet” which can satiate the requisites of an effective chemotherapeutic drug formulation. Pt(IV) complexes are kinetically more inert that the Pt(II) congeners and offer the opportunity to append additional functional groups/ligands for prodrug activation, tumor targeting or drug delivery. The ultimate aim for functionalization is to enhance the tumor selective action and attenuate systemic toxicity of the drugs. Moreover, increase in cellular accumulation to surmount the resistance of the tumor against the drugs is also of paramount importance in drug development and discovery. In this review, we will address some of the attempts in our lab to develop Pt(IV) prodrugs that can be activated and their targeted delivery using robust nanotechnology platforms.