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Updated: Mar 12, 2026

Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
Published on: November 10, 2013
Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present)
Peng-Cheng Lv, Zhong-Chang Wang, Hai-Liang Zhu1
1State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
Abstract:
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.
Insights
The c-Met receptor tyrosine kinase is crucial in aggressive cancers. This review details c-Met signaling, inhibitors, and their clinical development for targeted cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- c-Met (hepatocyte growth factor receptor) is a transmembrane receptor tyrosine kinase.
- Aberrant c-Met/HGF signaling is linked to aggressive cancer phenotypes, advanced disease, and poor prognosis.
- c-Met is an emerging target for cancer chemotherapy.
Purpose of the Study:
- To review signaling pathways of c-Met.
- To discuss c-Met crystal structures and ligand binding modes.
- To update on c-Met inhibitors developed since 2014, including clinical development and future prospects.
Main Methods:
- Literature review of signaling pathways.
- Analysis of published crystal structures and binding modes.
- Summary of inhibitor design, synthesis, SAR, and clinical trials.
Main Results:
- c-Met signaling pathways are implicated in aggressive cancers.
- Crystal structures reveal ligand binding mechanisms.
- Numerous c-Met inhibitors have been developed, with several in clinical trials.
Conclusions:
- c-Met is a validated therapeutic target in oncology.
- Ongoing development of c-Met inhibitors shows promise for cancer treatment.
- Future research directions focus on optimizing inhibitor efficacy and clinical application.
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