Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives
文献类型：期刊论文
| 作者 | Li, Jian; Tan, Jin-zhi; Chen, Li-li ; Zhang, Jian; Shen, Xu; Mei, Chang-lin; Fu, Li-li; Lin, Li-ping; Ding, Jian; Xiong, Bing
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2006-09 |
| 卷号 | 27期号:9页码:1259-1271 |
| 关键词 | 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 |
| 文献子类 | Article |
| 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. |
| WOS关键词 | EPIDERMAL-GROWTH-FACTOR ; TYROSINE KINASE INHIBITORS ; STRUCTURE-BASED DISCOVERY ; FACTOR RECEPTOR EGFR ; IRREVERSIBLE INHIBITORS ; CHEMICAL INHIBITORS ; BINDING-SITE ; PROTEIN ; DOMAIN ; DOCKING |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000240554800021 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273499]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物发现与设计中心 |
| 通讯作者 | Liu, Hong |
| 作者单位 | 1.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai Inst Mat Med,Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China 2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China 3.Second Mil Med Univ, Div Nephrol, Dept Internal Med, Changzheng Hosp, Shanghai 200003, Peoples R China 4.Shanghai Inst Mat Med, Div Antitumor Pharmacol, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jian,Tan, Jin-zhi,Chen, Li-li,et al. Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives[J]. ACTA PHARMACOLOGICA SINICA,2006,27(9):1259-1271. |
| APA | Li, Jian.,Tan, Jin-zhi.,Chen, Li-li.,Zhang, Jian.,Shen, Xu.,...&Jiang, Hua-liang.(2006).Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives.ACTA PHARMACOLOGICA SINICA,27(9),1259-1271. |
| MLA | Li, Jian,et al."Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives".ACTA PHARMACOLOGICA SINICA 27.9(2006):1259-1271. |
入库方式： OAI收割
来源：上海药物研究所
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