Antitumor Comparison of Three α-N-Heterocyclic Thiosemicarbazone Derivatives' Crystal Structures of Bis(2-acetylpyridine)thiocarbonohydrazone and Bis(imidazole-2-carboxaldehyde)thiocarbonohydrazone  

作　　者：陈春玲 陈丹云 李明雪 牛景杨 

机构地区：[1]Institute of Molecular and Crystal Engineering,College of Chemistry and Chemical Engineering,Henan University

出　　处：《Chinese Journal of Structural Chemistry》2010年第9期1380-1386,共7页结构化学（英文）

基　　金：supported by the Natural Science Foundation of Henan Province,the Natural Science Foundation of Educational Department of Henan Province (2010B150003);China Postdoctoral Science Foundation (20090460847)

摘　　要：A series of ligands,HL1（2-acetylpyridine thiosemicarbazone）,H2L2（bis（2-acetyl-pyridine） thiocarbonohydrazone） and H2L3（bis（imidazole-2-carboxaldehyde） thiocarbonohydrazone） was synthesized.H2L2 and H2L3 were characterized by elemental analysis,IR spectra and single-crystal X-ray diffraction studies.Hydrogen bonds link different components to stabilize the crystal structure in the two ligands.To comprehend the structure-activity relationship well,the three ligands are all tested against human K562 leucocythemia cell line with IC50 analysis.Different substituent groups on the ligands show different levels of antitumor activity.By comparison with the other species studied,H2L2 with thiocarbonohydrazone along with 2-acetylpyridine is the most active compound with IC50 = 2.48 μM.A series of ligands,HL1（2-acetylpyridine thiosemicarbazone）,H2L2（bis（2-acetyl-pyridine） thiocarbonohydrazone） and H2L3（bis（imidazole-2-carboxaldehyde） thiocarbonohydrazone） was synthesized.H2L2 and H2L3 were characterized by elemental analysis,IR spectra and single-crystal X-ray diffraction studies.Hydrogen bonds link different components to stabilize the crystal structure in the two ligands.To comprehend the structure-activity relationship well,the three ligands are all tested against human K562 leucocythemia cell line with IC50 analysis.Different substituent groups on the ligands show different levels of antitumor activity.By comparison with the other species studied,H2L2 with thiocarbonohydrazone along with 2-acetylpyridine is the most active compound with IC50 = 2.48 μM.

关 键 词：THIOSEMICARBAZONE thiocarbonohydrazone crystal structure cytotoxic activity 

分 类 号：R91[医药卫生—药学]