Synthesis, Characterization and Biological Activity of Diorganotin（IV） Complexes of N-（3,5-Dibromosalicylidene）-α-amino Acid  

作　　者：田来进 孙玉希 郑晓亮 刘希杰 于游 刘雪莉 钱伯初 

机构地区：[1]Department of Chemistry, Qufu Normal University, Qufu, Shandong 273165, China [2]Institute ofMateria Medica, Zhejiang Academy of Medical Science, Hangzhou, Zhejiang 310013, China [3]Institute of Chemistry, Chinese Academy of Sciences, Beijing 100080, China

出　　处：《Chinese Journal of Chemistry》2007年第3期312-318,共7页中国化学（英文版）

基　　金：Project supported by the Natural Science Foundation of Shandong Province （No. Z2002F01）, the State Key Laboratory of Crystal Materials （No. 2005B 103） and the Scientific Research Foundation of Qufu Normal University.

摘　　要：The diorganotin（Ⅳ） complexes of N-（3,5-dibromosalicylidene）-α-amino acid, R2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（where R=H, Me, i-Pr, Bz; R＇=n-Bu, Cy）, were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-（3,5-dibromosalicylidene）-α-amino acid and characterized by elemental analysis, IR and NMR （^1H, ^13C and ^119Sn） spectra. The crystal structures of n-Bu2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（R=i-Pr, Bz） and Cy2Sn（2-O-3,5-Br2C6H2CH=NCHRCOO）（R=Me, Bz） were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.The diorganotin（Ⅳ） complexes of N-（3,5-dibromosalicylidene）-α-amino acid, R2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（where R=H, Me, i-Pr, Bz; R＇=n-Bu, Cy）, were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-（3,5-dibromosalicylidene）-α-amino acid and characterized by elemental analysis, IR and NMR （^1H, ^13C and ^119Sn） spectra. The crystal structures of n-Bu2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（R=i-Pr, Bz） and Cy2Sn（2-O-3,5-Br2C6H2CH=NCHRCOO）（R=Me, Bz） were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.

关 键 词：organotin complex a-amino acid antitumour activity X-ray crystal structure 

分 类 号：R979.1[医药卫生—药品] R914.5[医药卫生—药学]