designsynthesisandantitumorevaluationofanewseriesofnsubstitutedthioureaderivatives
文献类型：期刊论文
| 作者 | Bing Xiong2 ; Xishan Xiong1; Hong Liu2; Xiaomin Luo2; Hualiang Jiang2; Jian Li2; Jinzhi Tan2; Lili chen2; Jian Zhang2; Xu Shen2
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| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2006 |
| 卷号 | 27期号:9页码:1259 |
| 关键词 | EPIDERMAL-GROWTH-FACTOR TYROSINE KINASE INHIBITORS STRUCTURE-BASED DISCOVERY FACTOR RECEPTOR EGFR IRREVERSIBLE INHIBITORS CHEMICAL INHIBITORS BINDING-SITE PROTEIN DOMAIN DOCKING N-substituted-thiourea derivatives anti-tumor SPAC1 tyrosine kinase inhibitor virtual screening |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2006.00437.x |
| 英文摘要 | Aim: To design and synthesize a novel class of protein tyrosine kinase inhibitors, featuring the N-(2-oxo-1,2-dihydroquinolin-3-yl-methyl)-thiourea framework. Methods: First, compounds 1 and 2 were identified using the virtual screening approach in conjunction with binding assay based on surface plasmon resonance. Subsequently, 3 regions of compounds 1 and 2 were selected for chemical modification. All compounds were characterized potent inhibitory activities toward the human lung adenocarcinoma cell line SPAC1. Results: Forty new compounds (1-2, 3a-g, 4a-w, and 5a-1) were designed, synthesized and bioassayed. Six compounds (1, 3e, 41, 4w, 5a, and 5b) were found to show promising inhibitory activity against the SPAC1 tumor cell line. The inhibitory activity of compound 5a increases approximately 10 times more than that of the original compound 1. Conclusion: This study provides a promising new template with potential antitumor activity. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/287351]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国人民解放军第二军医大学 2.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Bing Xiong,Xishan Xiong,Hong Liu,et al. designsynthesisandantitumorevaluationofanewseriesofnsubstitutedthioureaderivatives[J]. actapharmacologicasinica,2006,27(9):1259. |
| APA | Bing Xiong.,Xishan Xiong.,Hong Liu.,Xiaomin Luo.,Hualiang Jiang.,...&Jian Ding.(2006).designsynthesisandantitumorevaluationofanewseriesofnsubstitutedthioureaderivatives.actapharmacologicasinica,27(9),1259. |
| MLA | Bing Xiong,et al."designsynthesisandantitumorevaluationofanewseriesofnsubstitutedthioureaderivatives".actapharmacologicasinica 27.9(2006):1259. |
入库方式： OAI收割
来源：上海药物研究所
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