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Design, synthesis and molecular docking studies of some novel spiro[indoline-3, 4′-piperidine]-2-ones as potential c-Met inhibitors
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2012-02-18 , DOI: 10.1016/j.ejmech.2012.02.016
Lianbao Ye , Yuanxin Tian , Zhonghuang Li , Hong Jin , Zhengguang Zhu , Shanhe Wan , Junyan Zhang , Pengjiu Yu , Jiajie Zhang , Shuguang Wu

Deregulation of receptor tyrosine kinase c-Met has been reported in human cancers and is considered as an attractive target for small molecule drug discovery. In this study, a series of spiro[indoline-3, 4′-piperidine]-2-ones were designed, synthesized and evaluated as novel c-Met inhibitors. The results showed that the majority of the compounds exhibited significant inhibitory effect on c-Met with IC50 values of 0.0147–17 μM in TR-FRET-based assay and IC50 values of 1.56–1400 μM in cell-based assay. Furthermore, our docking experiments verified the results and explained the molecular mechanism of eminent activities to c-Met.



中文翻译:

一些新型螺[吲哚啉-3,4'-哌啶] -2-酮作为潜在的c-Met抑制剂的设计,合成和分子对接研究

受体酪氨酸激酶c-Met的失调在人类癌症中已有报道,被认为是发现小分子药物的诱人靶标。在这项研究中,设计,合成和评估了一系列螺[吲哚啉-3,4'-哌啶] -2-one,作为新型c-Met抑制剂。结果表明,大多数化合物显示对c-Met的带IC显著抑制效果50在基于TR-FRET的测定0.0147-17μM的值和IC 50个1.56-1400μM的值在基于细胞的测定。此外,我们的对接实验验证了结果并解释了c-Met突出活性的分子机制。

更新日期:2012-02-18
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