c-Met is a prototype member of a subfamily of heterodimeric receptor tyrosine kinases (RTKs) and is the receptor for hepatocyte growth factor (HGF). Binding of HGF to its receptor c-Met, initiates a wide range of cellular signalling, including those involved in proliferation, motility, migration and invasion. Importantly, dysregulated HGF/c-Met signalling is a driving factor for numerous malignancies and promotes tumour growth, invasion, dissemination and/or angiogenesis. Dysregulated HGF/c-Met signalling has also been associated with poor clinical outcomes and resistance acquisition to some approved targeted therapies. Thus, c-Met kinase has emerged as a promising target for cancer drug development. Different therapeutic approaches targeting the HGF/c-Met signalling pathway are under development for targeted cancer therapy, among which small molecule inhibitors of c-Met kinase constitute the largest effort within the pharmaceutical industry. The review is an effort to summarize recent advancements in medicinal chemistry development of small molecule c-Met kinase inhibitors as potential anti-cancer agents which would certainly help future researchers to bring further developments in the discovery of small molecule c-Met kinase inhibitors.

c-Met是异二聚体受体酪氨酸激酶（RTK）亚家族的原型成员，并且是肝细胞生长因子（HGF）的受体。HGF与其受体c-Met的结合引发广泛的细胞信号传导，包括那些参与增殖，运动，迁移和侵袭的信号传导。重要的是，HGF / c-Met信号传导失调是许多恶性肿瘤的驱动因素，并促进肿瘤生长，侵袭，扩散和/或血管生成。HGF / c-Met信号转导失调还与不良的临床结果和对某些批准的靶向疗法的耐药性产生相关。因此，c-Met激酶已成为癌症药物开发的有希望的靶标。针对HGF / c-Met信号通路的不同治疗方法正在针对靶向癌症治疗进行开发，其中c-Met激酶的小分子抑制剂构成了制药工业中最大的努力。该综述旨在总结小分子c-Met激酶抑制剂作为潜在的抗癌药物在药物化学发展方面的最新进展，这无疑将有助于未来的研究人员在发现小分子c-Met激酶抑制剂方面带来进一步的发展。