[1]王亚文,庄方方,律海峡,等.吲哚类化合物的制备及抗肿瘤活性研究[J].新乡医学院学报,2018,35(9):766-770.[doi:10.7683/xxyxyxb.2018.09.004]
　WANG Ya-wen,ZHUANG Fang-fang,LYU Hai-xia,et al.Synthesis and antitumor activity of indole compounds[J].Journal of Xinxiang Medical University,2018,35(9):766-770.[doi:10.7683/xxyxyxb.2018.09.004]
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吲哚类化合物的制备及抗肿瘤活性研究
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《新乡医学院学报》[ISSN:1004-7239/CN:41-1186/R]

卷:
35
期数:
2018年9
页码:
766-770
栏目:
基础研究
出版日期:
2018-09-05

文章信息/Info

Title:
Synthesis and antitumor activity of indole compounds
作者:
王亚文1; 庄方方2; 律海峡1; 闫福林1
（1.新乡医学院药学院，河南　新乡　453003；2.河南省职工医院药学部，河南　郑州　450001）
Author(s):
WANG Ya-wen1; ZHUANG Fang-fang2; LYU Hai-xia1; YAN Fu-lin1
（1.School of Pharmacy，Xinxiang Medical University，Xinxiang 453003，Henan Province，China；2.Department of Pharmacy，Henan Provincial Staff Hospital，Zhengzhou 450001，Henan Province，China）
关键词:
吲哚; 三级醇; 合成; 抗肿瘤活性
Keywords:
indole; tertiary alcohol; synthesis; antitumor activity
分类号:
R914
DOI:
10.7683/xxyxyxb.2018.09.004
文献标志码:
A
摘要:
目的　探索吲哚类化合物的制备及抗肿瘤活性，研发高效低毒的抗肿瘤药物。方法　以不同取代基的1，3-二羰基化合物为底物，与适量2，2，6，6-四甲基哌啶氧化物（TEMPO）反应生成α-位TEMPO取代的β-二羰基化合物中间体，再与吲哚或衍生物反应，制备含不同取代基的吲哚三级醇化合物，并用甲基噻唑基四唑法检测所合成的化合物对人神经母细胞瘤细胞SHSY5Y、食管癌细胞系109、乳腺癌细胞MCF、胃癌细胞MGC的半数抑制浓度（IC50）。结果　制备出8种含不同取代基的吲哚三级醇化合物，其中化合物7具有较好的细胞抑制作用。结论　建立了条件温和、收率高、操作简便的吲哚类化合物合成方法，为吲哚杂环三级醇类化合物的制备及后续的药理活性研究奠定了实验基础。
Abstract:
Objective　To investigate the preparation and antitumor activity of indole compounds，and to develop highly effective and low toxic antineoplastic agents.Methods　1，3-dicarbonyl compounds with different substituents were used as substrates to react with appropriate amount of 2，2，6，6-Tetramethylpiperidinooxy（TEMPO） to generate α-position TEMPO-substituted β-dicarbonyl compound intermediates，and then the indole tertiary alcohols containing different substituents were prepared by reacting with indole or derivatives.The half inhibitory concentration （IC50） of the compound on human neuroblastoma cell line SHSY5Y，esophageal cancer cell line 109，breast cancer cell MCF and gastric cancer cell MGC was detected by methylthiazolyl tetrazole （MTT） method.Results　Eight kinds of tertiary alcohol compounds with different substituents were prepared.The compound 7 has better cell inhibitory effect.Conclusion　The synthesis method of indole compounds has mild conditions，high yield and simple operation；which lays the experimental foundation for the preparation of the doped heterocyclic triols and their subsequent pharmacological activity.

参考文献/References:

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相似文献/References:

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　ZHUANG Fang-fang,YIN Yan-yan,YAN Jian-wei,et al.Synthesis and anti-tumor activity evaluation of indole-containing tertiary alcohols[J].Journal of Xinxiang Medical University,2016,33(9):267.[doi:10.7683/xxyxyxb.2016.04.005]

更新日期/Last Update: 2018-09-05