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新型含1,3,4-噁二唑啉的吡唑类化合物的合成及其抗肿瘤活性 被引量：2

Synthesis and Anti-tumor Activities of Novel Pyrazole Derivatives Containing 1,3,4-Oxadiazoline
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摘要 以4-甲氧基苯乙酮为原料,设计并合成了5个新型的含1,3,4-噁二唑啉的吡唑类化合物(6a^6e),其结构经1H NMR,13C NMR,IR和ESI-MS表征。用MTT法测定了6a^6e抑制人肝癌细胞Hep G2增殖的体外活性。结果表明:3-乙酰基-2-(4-乙酰氧基-3,5-二甲氧基苯基)-5-[3-(4-甲氧基苯基)-1-苯甲基-吡唑-5-基]噁二唑啉(6a)具有较好的抑制活性,其IC50为28.04μM,优于5-氟脲嘧啶(37.57μM)。 Five novel pyrazole derivatives containing 1,3,4-oxadiazoline（ 6a - 6e） were designed and synthesized from 4-methoxyacetophenone. The structures were characterized by1 H NMR,13^ C NMR,IR and ESI-MS. The in vitro anti-tumor activities of 6a - 6e were tested by MTT method. The results showed that 3-acetyl-2-（ 4-acetoxy-3,5-dimethoxyphenyl）-5-[3-（ 4-methoxyphenyl）-1-benzyl-pyrazol-5-yl]-oxadiazoline（ 6a） exhibited better inhibition activity against Hep G2 with IC50 of 28. 04 μM than5-FU（ 37. 57 μM）.
作者 张磊 王京 林娅 朱心玲 姚其正
机构地区 遵义医学院药学院 中国药科大学药学院
出处 《合成化学》 CAS CSCD 2015年第6期499-502,共4页 Chinese Journal of Synthetic Chemistry
基金 贵州省科技厅资助项目{黔科合LH字[2014]7565号 黔科合LH字[2014]7557号 黔科合人才团队[2014]4002号}
关键词 1 3 4-噁二唑啉 吡唑 合成 抗肿瘤活性 1 3 4-oxadiazoline pyrazole synthesis anti-tumor activity
分类号 O626.21 [理学—有机化学]
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参考文献11

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二级参考文献19

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合成化学
2015年 第6期

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