Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present)

Author(s): Peng-Cheng Lv, Zhong-Chang Wang, Hai-Liang Zhu

Journal Name: Current Medicinal Chemistry

Volume 24 , Issue 1 , 2017

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c-Met, also known as the surface receptor of hepatocyte growth factor receptor (HGFR), is a receptor tyrosine kinase with heterodimer transmembrane. c-Met involves in the activation of several signaling pathways, most of them are implicated in aggressive cancer phenotypes. In a variety of human malignances, c-Met/HGF signaling has been found aberrant, and in many instances, has been correlated with advanced disease stage and poor prognosis. Thus, the c-Met has identified as an emerging and interesting target for cancer chemotherapy. In this review, we briefly summarize signaling pathways of c-Met, and discuss the crystal structures of representative c-Met and the binding modes with their ligands. We also present updates on the design, synthesis and structure-activity relationship analysis of c-Met inhibitors developed from 2014 till now. At last, we review the c-Met inhibitors that are in clinical development and highlight the future prospects.

Keywords: c-Met inhibitors, hepatocyte growth factor receptor (HGFR), ATP-competitive inhibitors, anticancer agents, structure-activity relationship analysis, binding modes.

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Article Details

Year: 2017
Page: [57 - 64]
Pages: 8
DOI: 10.2174/0929867323666161028161441
Price: $65

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