具抗癌活性的茂环及β-二酮钛、锆和铪配合物的研究进展  

Research Progress in Cyclopentadienyl andβ-diketonato Titanium,Zirconium and Hafnium Complexes with Antitumor Activity

作　　者：王鹏[1] 赵添堃 姬明宇 杨明俊[1] 蒲秀瑛[1] Wang Peng;Zhao Tiankun;Ji Mingyu;Yang Mingjun;Pu Xiuying(College of Life Science and Engineering,Lanzhou University of Technology,Lanzhou,730050)

机构地区：[1]兰州理工大学生命科学与工程学院,兰州730050

出　　处：《化学通报》2021年第11期1163-1172,共10页Chemistry

基　　金：甘肃省自然科学基金项目(20JR5RA470)资助。

摘　　要：金属药物具有易制备、多价态、空间灵活及与生物靶标作用等优点,在抗癌药物的研究领域具有独特的优势。IVB族([钅卢]:放射性元素,本文不予讨论)金属配合物中的二氯二茂钛和布度钛作为抗癌潜力分子成功进入了临床试验,开创了药物化学的一个新篇章。虽然它们由于稳定性不足在临床试验中失败,但钛、锆和铪配合物因其优异的抗癌活性和低毒性仍得到了广泛的关注与研究。本文主要综述了茂环和β-二酮配位的钛、锆和铪及其衍生物的抗癌活性及结构-活性关系研究成果,尤其关注了近10年的进展,并对这两类配位体系下的钛、锆及铪配合物的未来发展方向做出了展望。Metal based drugs have many advantages such as easy preparation,multivalence,flexible space,the ability to react with biological targets,etc.,which are unique advantages in the field of anticancer drug research.Two titanium complexes,Titanocene dichloride and Budotitane,are the only two group IVB metal complexes(radioactive element Rutherfordium is not included)that have entered clinical trials as promising antitumor candidates,and they have opened a new chapter in medicinal chemistry.Despite the fact that they both failed in Phase II clinical trials because of their insufficient aqueous stability,titanium,zirconium and hafnium complexes still received much attention because of their good antitumor activity and low side effects.In this review,the anticancer activities and structure-activity relationships ofβ-diketonato and cyclopentadienyl titanium,zirconium and hafnium complexes and their derivatives are reviewed,especially the research progress of the last decade are presented.Meanwhile,the future perspectives of titanium,zirconium and hafnium complexes stabilized by these two ligand systems are stated.

关 键 词：金属配合物 二氯二茂钛 布度钛 β-二酮配体 抗癌活性 结构-活性 

分 类 号：O641.4[理学—物理化学] TQ460.1[理学—化学]