| 1,4-二氢噻吩并[3',2':5,6]噻喃并[4,3-c]吡唑-3-羧酸衍生物的合成及抗癌活性研究(英文) |
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| 引用本文： | 孙蕊,宋菁,赵辉,严春丽,张爱君,Koirala Diwa,李大伟,胡春. 1,4-二氢噻吩并[3',2':5,6]噻喃并[4,3-c]吡唑-3-羧酸衍生物的合成及抗癌活性研究(英文)[J]. 中国药学, 2011, 20(1): 32. DOI: 10.5246/jcps.2011.01.004 |
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| 作者姓名： | 孙蕊 宋菁 赵辉 严春丽 张爱君 Koirala Diwa 李大伟 胡春 |
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| 作者单位： | 沈阳药科大学制药工程学院基于靶点的药物设计与研究教育部重点实验室;上海交通大学药学院; |
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| 基金项目： | National Natural Science Foundation of China (Grant No. 20474053) |
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| 摘 要： | 本文以2-巯基噻吩为原料,经6步反应合成了5个1,4-二氢噻吩并[3',2':5,6]噻喃并[4,3-c]吡唑-3-羧酸衍生物,并采用人乳腺癌细胞MCF-7对目标化合物的抗肿瘤活性进行初步评价。所合成化合物在100μM浓度下均有一定的抑制MCF-7活性。
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| 关 键 词： | 合成 1 4-二氢噻吩并[3' 2':5 6]噻喃并[4 3-c]吡唑-3-羧酸衍生物 抗癌活性 |
Synthesis and anti-tumor activity of 1,4-dihydrothieno[3',2':5,6] thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives |
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| Rui Sun ,Jing Song ,Hui Zhao ,Chun-Li Yan ,Ai-Jun Zhang ,Diwa Koirala ,Da-Wei Li ,Chun Hu . Key Laboratory of Structure-Based Drug Design , Discovery,Ministry of Education,School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang ,China . School of Pharmacy,Shanghai Jiao Tong University,Shanghai ,China. Synthesis and anti-tumor activity of 1,4-dihydrothieno[3',2':5,6] thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives[J]. Journal of Chinese Pharmaceutical Sciences, 2011, 20(1): 32. DOI: 10.5246/jcps.2011.01.004 |
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| Authors: | Rui Sun Jing Song Hui Zhao Chun-Li Yan Ai-Jun Zhang Diwa Koirala Da-Wei Li Chun Hu . Key Laboratory of Structure-Based Drug Design Discovery Ministry of Education School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang China . School of Pharmacy Shanghai Jiao Tong University Shanghai China |
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| Affiliation: | Rui Sun 1,Jing Song 1,Hui Zhao 1,Chun-Li Yan 1,Ai-Jun Zhang 1,Diwa Koirala 2,Da-Wei Li 2,Chun Hu 1* 1. Key Laboratory of Structure-Based Drug Design and Discovery,Ministry of Education,School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China 2. School of Pharmacy,Shanghai Jiao Tong University,Shanghai 300193,China |
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| Abstract: | Five 1,4-dihydrothieno[3',2':5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives were synthesized from 2- mercaptothiophene via a six-step procedure. The prepared compounds were initially evaluated for their antiproliferative activity using the estrogen receptors expressing MCF-7 human mammary tumor cell line in vitro. All of the prepared compounds showed moderate anti-tumor activity. |
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| Keywords: | Synthesis 1 4-Dihydrothieno[3' 2':5 6]thiopyrano[4 3-c]pyrazole-3-carboxylic amide derivatives Anti-tumor activity |
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