新型三氮唑Schiff碱衍生物的合成及抗肿瘤活性研究（英文）

Synthesis and anti-tumor activities of novel triazole Schiff-base derivatives

以1-[二-(4-氟苯)甲基]哌嗪及氯乙酸乙酯为原料,经取代、肼解、环化制得3-[4-二-(4-氟苯)甲基哌嗪]-4-氨基-1,2,4-三氮唑-5-硫酮(5),5和取代芳香醛经缩合反应制得了22个Schiff碱6(a^v),其收率为73-85%。合成的22个目标化合物通过熔点测定和质谱、红外光谱、核磁共振氢谱分析、元素分析对其结构进行确证.经体外抗肿瘤活性测试表明除了化合物6(n,o)外,其余所有化合物均具有较好的活性,在化合物浓度为20ug/m L时,其抑制率高达99%。

Using 1-[bi-（4-fluorophenyl）-methyl]piperazine and ethyl chloroacetate as starting compound, 3-[4-bi-（4-fluorophenyl）-methylpiperazin-yl]-4-amino-1,2,4-triazole-5-thione（5） was synthesized through sequential reactions of substituation, hydrazinolysis and cyclization. Twenty-two novel triazole Schiff base 6（a-v） have been synthesized through compounds（5） reacted with substituted aromatic aldehydes under microwave irradiation with good yield（73-85%）. Their structures have been determined by elemental analysis, IR, MS and 1H NMR data. Preliminary bioassay indicated that all compounds exhibited good anti-tumor activities except the compounds 6（n,o）. At the concentration of 20μg/m L, the inhibition rates of compounds against CDC25 B were excellent（up to 99.8%）.