含桦木醇骨架的缩氨基硫脲及其金属配合物的合成

Betulin and its derivatives have anti-HIV activity, anti-tumor activity, and anti-inflammatory activities. More importantly, in anti-tumer and anti-AIDS, betulin derivatives have a different mechanism of action than other drugs, a good targeting efficiency, and little or no adverse reaction. The thiosemicarbazone structure for containing = NNH (C = S) - unit, can form complexes with a variety of metal ions, such metal complexes has anti-bacterial, anti-viral and anti-cancer activity. The = NNH (C = S) - unit combination to the betulin molecule, and then coordination with metal ions is possible to obtain compounds of higher activity. Metal complexes are known to exhibit a different activity with different of the metal ion, the ligands and types of coordination mode. This project intends design and synthesie of thiosemicarbazone ligand containing betulin skeleton, and determination of its anti-cancer, anti-bacterial activity. The focus of this project is on the clarification of the modes of metal-ligand coordination, screened new anti-cancer, anti-bacterial compound that low toxicity, high efficiency, low cost of the larger potential value. This study will provides a new idea in the search for antitumor and antibacterial substances, at the same time, can play a positive role in the development and utilization of the natural resources of our country.

桦木醇及其衍生物具有抗HIV、抗肿瘤和消炎等作用，更重要的是桦木醇和桦木酸类衍生物在抗肿瘤和抗HIV等方面显示出靶向作用强、不良反应小的特性。缩氨基硫脲结构中因含有=NNH(C=S)- 结构单元，能有效地与多种金属离子形成配合物，这种金属配合物具有抗菌、抗病毒、抗癌等活性。将=NNH(C=S)- 结构单元拼合到桦木醇分子中,再与金属离子配位有可能得到活性更高的化合物。金属配合物的活性研究中发现，金属离子、配体以及它们的配位模式不同则显示出不同的活性。本项目组拟合成含桦木醇骨架的缩氨基硫脲配体及其金属配合物，并测定其抗癌、抗菌活性。重点弄清配体与金属的配位模式，筛选出低毒、高效、价廉的有较大潜在利用价值的新的抗癌、抗菌化合物。这将对抗肿瘤和抗菌活性物质的研究提供新的思路，同时为我国天然资源的开发利用起到积极的作用。

桦木醇及其衍生物具有抗HIV、抗肿瘤和消炎等作用，更重要的是桦木醇和桦木酸类衍生物在抗肿瘤和抗HIV等方面显示出靶向作用强、不良反应小的特性。因此，已被视为很有前途的候选化合物，对其的研究已经成为近年来天然有机药物研究的热点。缩氨基硫脲及其金属配合物也具有抗肿瘤、抗菌等生物活性。本项目组利用拼合原理，拟合成含桦木醇骨架的缩氨基硫脲配体和其金属配合物，并通过抗肿瘤、抗菌活性实验筛选出新的高选择性、活性强及低毒的化合物，为研发新的抗癌和抗菌药物提供理论依据。