| 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
|
| リソース情報 |
| ヒト・動物細胞 |
|
