Recent Progress in the Development of Small Molecule c-Met Inhibitors

Author(s): Peng-Cheng Lv* , Yu-Shun Yang* , Zhong-Chang Wang* .

Journal Name: Current Topics in Medicinal Chemistry

Volume 19 , Issue 15 , 2019

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Graphical Abstract:


Abstract:

C-Met, also referred to as Hepatocyte Growth Factor Receptor (HGFR), is a heterodimeric receptor tyrosine kinase. It has been determined that c-Met gene mutations, overexpression, and amplification also occur in a variety of human tumor types, and these events are closely related to the aberrant activation of the HGF/c-Met signaling pathway. Meanwhile, high c-Met expression is closely associated with poor prognosis in cancer patients. The c-Met kinase has emerged as an attractive target for developing antitumor agents. In this review, we cover the recent advances on the small molecule c-Met inhibitors discovered from 2018 until now, with a main focus on the rational design, synthesis and structureactivity relationship analysis.

Keywords: c-Met, Tyrosine kinase, Small molecule inhibitors, Structure-activity relationship analysis, Anticancer agents, Drug development.

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