| Literature DB >> 23702473 |
Lianbao Ye1, Xiaomin Ou, Yuanxin Tian, Bangwei Yu, Yan Luo, Binghong Feng, Hansen Lin, Jiajie Zhang, Shuguang Wu.
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.Entities:
Keywords: AQKULDWMVLPKPM-RQNOJGIXSA-N; ASSDAYRAIJUAKP-UHFFFAOYSA-N; Bioisosterism principles; IOEGMAJBPLCGLZ-RQNOJGIXSA-N; Indazole; Isomer; KFHKXMBLOGYCPH-OGESRWMOSA-N; KUZAYSZLNQTGIG-UHFFFAOYSA-N; LNULRIFOOHDLKU-UHFFFAOYSA-N; Molecular docking; QONCLFMRNBSJDL-UHFFFAOYSA-N; SGCGRBMTXZLJBR-OGESRWMOSA-N; Suzuki coupling reaction; VMWYPUTZWINMTO-UHFFFAOYSA-N; VXDNOGKPNKBTFZ-UHFFFAOYSA-N; c-Met inhibitor
Mesh：
Substances：
Year: 2013 PMID： 23702473 DOI： 10.1016/j.ejmech.2013.04.004
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514