| 新型三环肟醚衍生物的合成及其抗肿瘤活性 |
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| 引用本文： | 郭淑春,陈阳,张珂良,王伟,李伟,宫平.新型三环肟醚衍生物的合成及其抗肿瘤活性[J].中国药物化学杂志,2007,17(5):274-278. |
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| 作者姓名： | 郭淑春 陈阳 张珂良 王伟 李伟 宫平 |
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| 作者单位： | 1. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016
2. 辽宁省食品药品监督管理局,技术审评中心,辽宁,沈阳,110003 |
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| 摘 要： | 目的设计合成8H-噻吩并2,3-b]吡咯里嗪-8-肟醚类化合物,并对其体外抗肿瘤活性进行初步评价。方法以芳基乙腈为原料,经多步反应合成目标化合物;采用MTT法,以顺铂为阳性对照药,以Bel-7402和HT-1080为测试细胞株对目标化合物的抗肿瘤活性进行了评价。结果与结论合成了12个新化合物,经1H-NMR、MS和IR确认其结构。体外活性实验表明:化合物7d显示出较好的抗肿瘤活性。
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| 关 键 词： | 8H-噻吩并[2 3-b]吡咯里嗪类化合物 抗肿瘤活性 微管蛋白抑制剂 |
| 文章编号： | 1005-0108（2007）05-0274-05 |
| 收稿时间： | 2007-03-28 |
| 修稿时间： | 2007年3月28日 |
Synthesis and antitumor activities of novel tricyclic oximino derivatives |
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| GUO Shu-chun,CHEN Yang,ZHANG Ke-liang,WANG Wei,LI Wei,GONG Ping.Synthesis and antitumor activities of novel tricyclic oximino derivatives[J].Chinese Journal of Medicinal Chemistry,2007,17(5):274-278. |
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| Authors: | GUO Shu-chun CHEN Yang ZHANG Ke-liang WANG Wei LI Wei GONG Ping |
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| Institution: | 1. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China ; 2. Liaoning FDA Technical Evaluation Center, Shenyang 110003, China |
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| Abstract: | Aim To design and synthesize a series of novel thieno 2,3-b]pyrrolizine derivatives,and to evaluate their antitumor activities.Methods Twelve target compounds were synthesized in several steps with the starting material arylacetonitrile and their antitumor activities were examined against Bel-7402 and HT-1080 cell lines in vitro with cisplatin as positive control.Results and conclusion The structures of twelve new compounds were confirmed by 1H-NMR,IR,and MS.The pharmacological tests showed that compound 7d showed promising antitumor activity. |
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| Keywords: | thieno[2 3-b]pyrrolizines antitumor activities tubulin inhibitor |
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