| 3-取代-5-氟-1-2-二氢-3H-吲哚-2-酮类化合物的合成及抗肿瘤活性 |
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| 引用本文： | 陈重,李钦,樊后兴.3-取代-5-氟-1-2-二氢-3H-吲哚-2-酮类化合物的合成及抗肿瘤活性[J].中国医药工业杂志,2009,40(10). |
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| 作者姓名： | 陈重 李钦 樊后兴 |
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| 作者单位： | 陈重,李钦(河南大学中药研究所,河南开封,475004);樊后兴(上海阳帆医药科技有限公司,上海,201203) |
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| 摘 要： | 5-溴-1H-吲哚经氰基取代、Vilsmeier-Haack反应、水解、缩合制得3-(Z)-(5-氟-1,2-二氢-2-氧代-3H-亚吲哚基)甲基]-1H-吲哚-5-甲酸,再和相应的胺类化合物反应制得10个3-取代-5-氟-1,2-二氢-3H-吲哚-2-酮类化合物.以舒尼替尼为阳性对照,用MTT法测试目标化合物对人乳腺上皮细胞HMEC的体外抑制活性,其中1c、1f、1g和1h在浓度为10 μmol/L时,对HMEC的抑制活性优丁舒尼替尼.进一步测试1c和1e对SGC7901、A549、HL-60、SK-BR-3、HCT116肿瘤细胞株的抗增殖活性.结果表明,1c和1e对白血病细胞株HL-60的抗增殖活性优丁舒尼替尼.
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| 关 键 词： | 3-取代-5-氟-1 2-二氧-3H-吲哚-2-酮 血管生成抑制剂 合成 抗肿瘤活性 |
Synthesis and Antitumor Activities of 3-Substituted-5-fluoro-1,2-dihydro-3H-indol-2-ones |
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| Abstract: | Started from 5-bromo-1H-indole, a series of new 3-substituted-5-fluoro-1,2-dihydro-3H-indol-2-ones were synthesized via cyanation, Vilsmeier-Haack reaction, hydrolysis and condensation to give 3- (Z) - (5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl]-1H-indole-5-carboxylic acid, which was subjected to amination with the substituted amine. The in vitro antitumor activities of ten target compounds were evaluated against HMEC cell lines by MTT method with sunitinib as a positive control, and 1c, 1f, 1g and 1h showed better inhibitory activity against HMEC than sunitinib at the concentration of 10 祄ol/L. Compounds 1c and 1e were selected to further evaluation on their anti-proliferation activities against SGC7901, A549, HL-60, SK-BR-3, HCT116 cell lines, the result showed that 1c and 1e had more potent anti-proliferation activities than sunitinib against HL-60 cell. |
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| Keywords: | 3-substituted-5-fluoro-l 2-dihydro-3H-indol-2-one antiangiogenic agent synthesis antitumor activity |
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