Antitumor Comparison of Three α-N-Heterocyclic Thiosemicarbazone Derivatives' Crystal Structures of Bis(2-acetylpyridine)thiocarbonohydrazone and Bis(imidazole-2-carboxaldehyde)thiocarbonohydrazone |
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作者姓名: | CHEN Chun-Ling CHEN Dan-Yun LI Ming-Xue NIU Jing-Yang |
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作者单位: | Institute of Molecular and Crystal Engineering, College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004, China |
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基金项目: | 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) |
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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.
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关 键 词: | 酰氨基硫脲 晶体结构 乙酰基 硫脲衍生物 咪唑 甲醛 抗癌 杂环 |
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