| 温倩雯,黎勇,苏正颖,万丽.化学通报,2019,82(4):350-358. |
| 4-(5H-嘧啶并[5,4-b]吲哚-2-氨基)苯甲酰胺类化合物的设计、合成及抗肿瘤活性研究 |
| Design and synthesis of 4-(5H-pyrimido[5,4-b]indole-2-amino)benzamide derivatives as antitumor agents |
| 投稿时间：2018-11-01 修订日期：2018-12-20 |
| DOI： |
| 中文关键词: 嘧啶并吲哚,苯甲酰胺,合成,抗肿瘤活性 |
| 英文关键词:9H-pyrimido[4,5-b]indole, benzamide, synthesis, anti-tumor activity |
| 基金项目:国家自然科学基金项目（基金项目号） |
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| 摘要点击次数: 1554 |
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| 中文摘要: |
| 设计、合成了19个未见文献报道的4-(5H-嘧啶并[5,4-b]吲哚-2-氨基)苯甲酰胺类衍生物,所合成的化合物均经1H NMR, 13C NMR 及HRMS 确认。并采用噻唑蓝(MTT)法测试了目标化合物对人结肠癌细胞(HCT116)、人乳腺癌细胞(MD-MBA-231)、大鼠神经胶质瘤细胞(C6)、人非小细胞肺癌细胞(A549)、人乳腺癌细胞(MCF-7)的体外抗肿瘤活性。结果表明,所有化合物均表现出较好的抗肿瘤活性。其中5a、5b、5c、5e、5i、5p和5r对多个细胞株的抑制活性为阳性对照药品5-氟尿嘧啶的20~100倍,以5b的抗肿瘤活性最为突出,对肿瘤细胞HCT116、MD-MBA-231、C6、A549、MCF-7的IC50分别为3.26、3.06、0.63、0.68、2.32 μmol/L。初步的体外抗肿瘤活性研究表明,此类化合物对肿瘤细胞增殖有明显抑制作用,具有潜在的继续研究价值,为新型抗肿瘤化合物的设计、合成提供思路。 |
| 英文摘要: |
| 19 novel 4-(5H-pyrimido[5,4-b]indol-2-amino)benzamine derivatives were synthesized and evaluated for their in vitro antiproliferative activity. All of the title compounds were confirmed by 1H NMR, 13C NMR and HRMS. The anti-tumor activity of the title compounds against HCT116, MD-MBA-231, C6, A549 and MCF-7 cancer cell lines were tested by MTT assay. The results showed that all compounds had good anti-tumor activity, especially compounds 5a, 5b, 5c, 5e, 5i, 5p and 5r, showed 20 to 100 folds activity enhancement than the positive control 5-fluorouracil. 5b was the most potential one among them, whose IC50 of HCT116, MD-MBA-231, C6, A549 and MCF-7 were 3.26, 3.06, 0.63, 0.68 and 2.32 μmol/L. These findings suggested that these derivatives have a significant inhibitory effect on tumor cells proliferation, which laid the foundation to design and synthesize new 5H-pyrimido[5,4-b]indol-2-amine based derivatives as anti-tumor compounds, providing advices to the pharmaceutical researchers. |
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