糠酰异羟肟酸类有机锡配合物的合成及其抗癌活性  

Synthesis and antitumor activities of diorgano,dichloro-tin(Ⅳ) complexes of furohydroxamates

作　　者：赵敬华[1] 李青山[1] 

机构地区：[1]山西医科大学药学院

出　　处：《中国药物化学杂志》2006年第6期347-351,共5页Chinese Journal of Medicinal Chemistry

基　　金：国家教育部新世纪优秀人才支持计划项目(NCET-04-0258);山西省首批中青年学科带头人基金项目(晋教科200413)

摘　　要：目的设计合成糠酰异羟肟酸类有机锡配合物,并进行抗癌活性测定。方法首先合成糠酰异羟肟酸(FuHA),并以之为配体合成一系列二烃基锡配合物;运用MTT法进行糠酰异羟肟酸类有机锡配合物对血癌K562细胞和骨髓瘤细胞EP-20的体外抗癌活性筛选。结果合成了1个配体和5个配合物,用熔点、元素分析、FT-IR1、H-NMR和13C-NMR等方法进行了结构表征,R2Sn(L)2型化合物为六配位畸变八面体,而[R2Sn(L)]2O型化合物为五配位双核三角双锥结构。结论正丁基锡和苯基锡配合物具有明显的抗癌活性。Aim To design and synthesize diorgano, dichloro-tin （Ⅳ） complexes of furohydroxamates and evaluate their antitumor activities. Methods A series of diorganotin （Ⅳ） furohydroxamates formulated as R2Sn（L）2 or [R2Sn（L）]2O with furohydroxamatic acid （FuHA） as the ligand were prepared. Their antitumor activity against leucocythemia K562 cell and marrow tumor EP-20 cell in vitro was tested by MTT method. Results One ligand and five complexes were synthesized and characterized by melting point, element analysis, FT-IR, ^1H-NMR, and ^13C-NMR. Conclusion The di（n-butyl） tin and diphenyltin complexes have strong antitumor activity in vitro.

关 键 词：药物化学 化合物制备 化学合成 有机锡配合物 糠酰异羟肟酸 抗癌活性 

分 类 号：R914[医药卫生—药物化学]