| 3-取代氧化吲哚的合成及其抗肿瘤活性研究 |
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| 引用本文： | 黄璇,景德红,俸婷婷,郭丰敏,周英,刘雄利,余章彪.3-取代氧化吲哚的合成及其抗肿瘤活性研究[J].贵州大学学报(自然科学版),2014,31(6):34-37. |
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| 作者姓名： | 黄璇 景德红 俸婷婷 郭丰敏 周英 刘雄利 余章彪 |
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| 作者单位： | 贵州大学药学院贵州省中药民族药创制工程中心,贵州贵阳,550025 |
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| 基金项目： | 国家青年基金资助项目，贵州省中药现代化科技产业研究开发专项项目，贵州省教育厅课题，贵州民族药物中新颖活性组分的结构测定及NMR谱仪的应用研发项目 |
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| 摘 要： | 以不同取代的靛红为起始原料,通过和各种取代基的格式试剂反应生成3-羟基化氧化吲哚中间体,然后在氮原子和氧原子上用Boc保护,再在Pd/C条件下氢气脱OBoc,即得到3-取代-N-叔丁氧羰基氧化吲哚（3a ～3g）,总产率为52％～67％,讨论了底物取代基对反应产率的影响.结构经1H NMR,13C NMR和HRMS表征.采用MTT法研究了3a ～3g体外对前列腺癌细胞（PC-3）的抗肿瘤活性.结果表明：5-氟-3-苯基-N-叔丁氧羰基氧化吲哚（3d）对PC-3具有较好的抑制活性.
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| 关 键 词： | 3-取代氧化吲哚 靛红 PC-3 抗肿瘤 |
The Synthesis and Anti-Tumor Activity of 3-Substituted Oxindoles |
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| HUANG Xuan,JING De-hong,FENG Ting-ting,GUO Feng-min,ZHOU Ying,LIU Xiong-li,YU Zhang-biao.The Synthesis and Anti-Tumor Activity of 3-Substituted Oxindoles[J].Journal of Guizhou University(Natural Science),2014,31(6):34-37. |
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| Authors: | HUANG Xuan JING De-hong FENG Ting-ting GUO Feng-min ZHOU Ying LIU Xiong-li YU Zhang-biao |
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| Institution: | ( Guizhou Engineering Center for Innovative Traditional Chinese Medicine and Ethnic Medicine, College of Pharmacy, Guizhou University, Guiyang 550025, China) |
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| Abstract: | The paper starts with the different substituted isatins reaction with different Grignard reagent to get 3- hydroxymethyl-oxindole intermediates, then introduces the Boc as protection group in the nitrogen and oxygen at- oms, eliminates the OBoe through reaction with hydrogen under the condition of Pd/C, finally to obtain the 3- monosubstituted oxindole（3a-3g）, the yields were 52% -67%, the effects of different substrates were also discussed. All the ultimate compounds were confirmed by 1H NMR and 13C NMR. The compounds＇ antineo- plastic activity was valuated for cytotoxicity against human prostatic cancer cell（ PC-3 ） by MTT method. The re- sults demonstrated that these compounds had the activity of inhibition on the PC-3 cancer cells, especially 3d possessed higher anti-tumor activity. |
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| Keywords: | 3-substituted oxindole isatin PC-3 anti-tumor |
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