designsynthesisantitumorevaluationsandmolecularmodelingstudiesofnovel35substitutedindolin2onederivatives
文献类型：期刊论文
| 作者 | Luo Xiaomin ; Shen Xu; Lin Liping; Chen Kaixian; Li Haihong; Zhang Xiuhua; Tan Jinzhi; Chen Lili; Liu Hong; Ding Jian
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2007 |
| 卷号 | 28期号:1页码:140 |
| 关键词 | Protein-tyrosine kinase Indolin-2-one Antitumor drug screening assays Drug design Molecular models |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim: To design and synthesize a novel class of antitumor agents, featuring the 3,5-substituted indolin-2-one framework. Methods: Based on enzyme binding features of (Z)-SU5402, introducing a b-pyrrole group at the 3-position of the indolin-2-one core, a series of novel 3,5-substituted indolin-2-ones were designed and synthesized. Four human carcinoma cell lines of A-431, A-549, MDA-MB-468, and Autosomal Dominant Polycystic Kidney disease were chosen for the cell proliferation assay. Results: Twenty new compounds (1a_t) with E configuration have been designed, synthesized and bioassayed. Their structural features were determined by nuclear magnetic resonance (NMR) spectra, low- and high-resolution mass spectra, and confirmed by X-ray crystallography. Although the enzyme assay showed a weak inhibition effect against the epidermal growth factor receptor, vascular endothelial growth factor receptor, fibroblast growth factor receptor and platelet-derived growth factor receptor tyrosine kinases, the cell-based antitumor activity was promising. Compounds 1g and 1h showed higher inhibitory activity toward the A-549 and MDA-MB-468 cell lines with IC_(50)of 0.065_9.4 μmol/L. Conclusion: This study provides a new template for further development of potent antitumor drugs. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/287368]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Luo Xiaomin,Shen Xu,Lin Liping,et al. designsynthesisantitumorevaluationsandmolecularmodelingstudiesofnovel35substitutedindolin2onederivatives[J]. actapharmacologicasinica,2007,28(1):140. |
| APA | Luo Xiaomin.,Shen Xu.,Lin Liping.,Chen Kaixian.,Li Haihong.,...&Jiang Hualiang.(2007).designsynthesisantitumorevaluationsandmolecularmodelingstudiesofnovel35substitutedindolin2onederivatives.actapharmacologicasinica,28(1),140. |
| MLA | Luo Xiaomin,et al."designsynthesisantitumorevaluationsandmolecularmodelingstudiesofnovel35substitutedindolin2onederivatives".actapharmacologicasinica 28.1(2007):140. |
入库方式： OAI收割
来源：上海药物研究所
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