新型抗癌双核铂配合物的设计、合成及构效关系研究

With the purpose of finding novel antitumor bridged binuclear platinum complexes, this project, proceeding from molecular designing, is to design and clip ligands and synthesize a series of novel orienting bridged binuclear platinum(II,IV) complexes with different bridging and terminal ligands via synthetic methods of modern coordination chemistry. After determining the structures of these complexes, their antitumor activities will be evaluated. The coordination effect between bridging and terminal ligands and the effect of molecular structures and platinum on different valence states on antitumor activities will be studied systematically and intensively.This to analyze the mechanism of antitumor. The structure activity relationship will also be discussed by comparing the antitumor activities of different binuclear platinum complexes, and novel antitumor binuclear platinum complexes with less cytotoxicities and high activities and selectivities will be selected to provide a basis for the development of the metal-based antitumor drugs. This project will open a new field to develop effective antitumor complexes and its findings will be of great theoretical significance and of a valuable application prospect.

本项目以寻找具有抗癌活性的新型桥联双核铂配合物为目标，从分子设计出发，通过对配体的设计和剪裁，并应用现代配位化学合成技术手段，定向合成一系列含有不同桥基和端基配体的新型桥联双核铂(II、IV)配合物；测定它们的结构及抗癌活性；在深入系统研究桥基配体和端基配体的协调效应、铂的不同价态及分子结构对抗癌活性影响的基础上，剖析其抗癌机理；通过对所合成的一系列双核铂配合物的结构与抗癌活性的对比分析，探讨构效关系，并从中筛选出活性和选择性高、毒副作用小的新型抗癌双核铂配合物，为金属抗癌药物的研制提供科学依据。该项目的实施开辟了抗癌活性配合物研究的新途径，其研究结果具有重要的理论意义和潜在应用前景。

本项目以寻找具有抗癌活性的新型桥联双核配合物为目标，从分子设计出发，通过对配体的设计和剪裁，并应用现代配位化学合成技术手段，定向合成一系列含有不同桥基和端基配体的新型桥联双核配合物；测定它们的结构及抗癌活性；在深入系统研究桥基配体和端基配体的协调效应、金属的不同价态及分子结构对抗癌活性影响的基础上，剖析其抗癌机理；通过对所合成的一系列双核铂配合物的结构与抗癌活性的对比分析，探讨构效关系，并从中筛选出活性和选择性高、毒副作用小的新型抗癌双核配合物，为金属抗癌药物的研制提供科学依据。该项目的实施开辟了抗癌活性配合物研究的新途径，其研究结果具有重要的理论意义和潜在应用前景。