論文 - 詳細
| RRC ID | 44453 |
|---|---|
| 著者 | Ye L, Ou X, Tian Y, Yu B, Luo Y, Feng B, Lin H, Zhang J, Wu S. |
| タイトル | Indazoles as potential c-Met inhibitors: design, synthesis and molecular docking studies. |
| ジャーナル | Eur J Med Chem |
| Abstract |
Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is considered as an attractive target for small molecule drug discovery. In this study, a series of indazoles were designed, synthesized and evaluated as novel c-Met inhibitors. The results showed that the majority of the compounds exhibited significant inhibition on c-Met and compound 4d showed highest activity against c-Met with IC50 value of 0.17 μM in TR-FRET-based assay and IC50 value of 5.45 μM in cell-based assay as compared to other tested compounds. Molecular docking experiments verified the results and explained the molecular mechanism of pretty activities to c-Met. |
| 巻・号 | 65 |
| ページ | 112-8 |
| 公開日 | 2013-7-1 |
| DOI | 10.1016/j.ejmech.2013.04.004 |
| PII | S0223-5234(13)00236-5 |
| PMID | 23702473 |
| MeSH | Cell Line, Tumor Dose-Response Relationship, Drug Drug Design* Humans Indazoles / chemical synthesis Indazoles / chemistry Indazoles / pharmacology* Models, Molecular Molecular Structure Protein Kinase Inhibitors / chemical synthesis Protein Kinase Inhibitors / chemistry Protein Kinase Inhibitors / pharmacology* Proto-Oncogene Proteins c-met / antagonists & inhibitors* Proto-Oncogene Proteins c-met / metabolism Structure-Activity Relationship |
| IF | 5.573 |
| 引用数 | 22 |
| WOS 分野 | CHEMISTRY, MEDICINAL |
| オルトメトリクス指標 |
オルトメトリクス指標項目
|
| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 4 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | |