铂类抗肿瘤药物的设计开发进展

Design and development progress of platinum-based anticancer drugs

铂类抗肿瘤药物是临床上使用广泛的化疗药物,具有近40年的研究和使用历史.本文对临床上使用和处于临床研究中的铂类药物进行了简单介绍,总结了进入临床研究阶段被淘汰的铂类药物,针对目前铂类药物所处形势重点介绍了新一代铂类药物的设计开发方法.新一代铂类药物包括修饰和改进的经典构型的Pt(II)配合物、反式Pt(II)配合物、药物前体Pt(IV)配合物、单功能铂配合物、配位饱和的铂配合物和多核铂配合物等.通过列举最新研究成果,分析药物作用机制,提出铂类药物的设计开发方法,让读者了解铂类抗肿瘤药物的发展历程和未来的发展趋势.

Platinum-based anticancer drugs which are widely used in clinic have nearly 40 years history of research and application. In this review, we make a brief introduction of platinum-based anticancer drugs which have been used in clinic or still during the clinical trails, and summarized the drugs which were failed in clinical trails. We introduce the design and development methods of new generation platinum-based anticancer drugs consisting of platinum（II） complexes such as modified and improved trans-platinum（II） complexes, platinum（IV） complexes, and mono-functional platinum complexes. Coordination-saturation platinum complexes and multinuclear platinum complexes are discussed emphatically. This review has put forward some design methods of platinum-based anticancer drugs through listing some of the latest research results, and let readers understand the development of platinum-based anticancer drugs and the future direction of development.