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α-N-杂环羧醛缩氨基硫脲铁(II)和铁(III)配合物的合成、表征及抗肿瘤活性

Synthesis, characterization, and antitumor activity of iron(II) and iron(III) complexes of alpha-N-heterocyclic carboxaldehyde thiosemicarbazones.

作者信息

Mohan M, Kumar M, Kumar A, Madhuranath P H, Jha N K

机构信息

Department of Chemistry, N.R.E.C. College, Khurja, India.

出版信息

J Inorg Biochem. 1988 Apr;32(4):239-49. doi: 10.1016/0162-0134(88)85003-7.

Abstract

Complexes of iron(II) and iron(III) with 1-formylisoquinoline thiosemicarbazone (1-iqtsc-H), 4-methyl-5-amino-1-formylisoquinoline thiosemicarbazone (4-Me-5-NH2-1-iqtsc-H) and 4-(m-aminophenyl)-2-formylpyridine thiosemicarbazone (4-m-NH2ph-2-pytsc-H) were synthesized and characterized by elemental analysis, conductance measurements, magnetic susceptibilities (from room temperature down to liquid N2 temperature), and Mössbauer, electronic, and infrared spectral studies. On the basis of these studies, a highly distorted, high-spin, five-coordinate structure for Fe(HL)SO4 (HL = 1-iqtsc-H, 4-Me-5-NH2-1-iqtsc-H or 4-m-NH2ph-2-pytsc-H) and a distorted, low-spin, octahedral structure for Fe(HL)Cl2 are suggested. The EPR spectra of iron(III) complexes show that all have dxy low-spin ground state. All these complexes have been screened for their antitumor activity against the P 388 lymphocytic leukemia test system in mice and have been found to possess significant activity at the dosages employed.

摘要

合成了铁(II)和铁(III)与1-甲酰基异喹啉硫代半卡巴腙(1-iqtsc-H)、4-甲基-5-氨基-1-甲酰基异喹啉硫代半卡巴腙(4-Me-5-NH2-1-iqtsc-H)以及4-(间氨基苯基)-2-甲酰基吡啶硫代半卡巴腙(4-m-NH2ph-2-pytsc-H)的配合物,并通过元素分析、电导率测量、磁化率(从室温到液氮温度)以及穆斯堡尔谱、电子光谱和红外光谱研究对其进行了表征。基于这些研究,推测Fe(HL)SO4(HL = 1-iqtsc-H、4-Me-5-NH2-1-iqtsc-H或4-m-NH2ph-2-pytsc-H)具有高度扭曲的高自旋五配位结构,而Fe(HL)Cl2具有扭曲的低自旋八面体结构。铁(III)配合物的电子顺磁共振光谱表明,所有配合物都具有dxy低自旋基态。所有这些配合物都针对小鼠P 388淋巴细胞白血病测试系统进行了抗肿瘤活性筛选,发现在所用剂量下具有显著活性。

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