粘着斑激酶（FAK）是一种在多种恶性肿瘤中过度表达的细胞质非受体酪氨酸激酶，与粘附、转移和增殖等多种细胞功能相关。越来越多的证据表明，FAK 是通过调节 FAK 下游通路来设计抑制剂的有前途的治疗靶点。在此，我们基于之前的工作，更新了2017年至今化疗FAK抑制剂（FAKI）的设计、合成和结构-活性关系的概述。我们希望我们的努力能够拓宽对FAKI的理解，并从药物化学的角度为未来的癌症治疗提供新的思路和见解。

Focal adhesion kinase (FAK) is a cytoplasmic non-receptor tyrosine kinase over-expressed in various malignancies which is related to various cellular functions such as adhesion, metastasis and proliferation. There is growing evidence that FAK is a promising therapeutic target for designing inhibitors by regulating the downstream pathways of FAK. Here, we updated an overview of design, synthesis and structure - activity relationship of chemotherapeutic FAK inhibitors (FAKIs) from 2017 until now based on our previous work. We hope our efforts can broaden the understanding of FAKIs and provide new ideas and insights for future cancer treatment from medicinal chemistry point of view.