| 陈仕杰,龚显峰,沈明辉,王雪微,张华.化学通报,2015,78(7):621-626. |
| 伊马替尼衍生物的合成及细胞毒活性研究 |
| Synthesis and cytotoxic activity of imatinib derivative |
| 投稿时间：2014-11-23 修订日期：2014-12-26 |
| DOI： |
| 中文关键词: 伊马替尼衍生物 合成 MTT法 |
| 英文关键词:Imatinib derivatives Synthesis MTT assay |
| 基金项目: |
|
| 摘要点击次数: 2456 |
| 全文下载次数: 0 |
| 中文摘要: |
| 本文以3-乙酰基嘧啶、2-甲基-5-硝基苯胺为起始原料,经加成、缩合、环化、还原得到中间体伊马替胺(6),再与异氰酸酯和芳酰基异硫氰酸酯胺解得到脲类(7a~7e)和芳酰基硫脲类(8a~8g)共计12个化合物。目标化合物经过IR、1HNMR、13CNMR、HRMS等结构确证。采用四甲基偶氮唑盐(MTT)法考察目标化合物细胞毒活性, 结果显示目标化合物对所选肿瘤细胞的增殖抑制活性不高, 其中化合物7d、7e、8d对人白血病细胞(K562)和人肝癌细胞(HepG2)的抑制活性接近伊马替尼。 |
| 英文摘要: |
| A series of novel imatinib derivatives urea(7a~7e) and aroyl thiourea (8a~8g) were synthesized using 3-acetyl-pyrimidin, and 2-methyl-5-nitroaniline as starting material via addition reaction, condensation, cyclization, reduction reaction, then reaction with isocyanate and isothiocyanate. The structures of all target compounds were confirmed by IR, 1H NMR, 13C NMR and HRMS, they were evaluated for cytotoxic activity against human Leukemia cells(K562) lines and human hepatoma cell line(HepG2) by methyl thiazolyl tetrazolium (MTT) method, It shows that they have certain inhibitory activity, especially compounds 7d、7e、8d have approximation inhibitory activity on K562 and HepG2 with imatinib. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|