新型有机锡类抗癌先导化合物的优化及其作用机制研究

In this project, structure optimizations of the novel antitumor diorganotin lead compound were investigated. Three series of new diorganotin compounds, nearly one hundred were thus prepared and were structurally characterized by FT-IR、1H、13C、119Sn NMR、Mass spectra and X-ray methods.The in vitro antitumor activity experiments were carried out and the in vivo activity tests and acute toxicity study of two novel diorganotin compounds, DBDCT, DBDNT with high in vitro acvitity were further investigated along with the further action mechanism study. The results show that DBDCT and DBDNT not only exhibite strong in vivo activity against gastric carcinoma and liver tumor but also have relatively low toxicity and special action mechanism, their cure rate is over 20 and thus, show great potential clinical value. All the results provided further scientific support for the design principle put forward by the research group which maybe be used in the investigation of other metal-based antitumor compounds. Ten papers about the achievements of the project were published in famous international and national academic journals and five patents were applied for the approval of China and European. Two First Class Prizes of Science and Technology Progress of Shanxi Province were awarded to the researchers.

本项目拟进一步设计机合成一系列新型有机锡类抗癌化合物，通过体内外抗癌作用研究和毒理研究，筛选出抗癌活性高、毒性较低、有重要临床应用前景的有机锡抗癌剂，并从分子水平上阐明其抗癌作用机制。对癌症化疗新药的开发研究有重要的理论价值和应用前景。