Kinases are pivotal regulators in tumorigenesis and metastasis by modulating the expression of oncogenes and the transcription of antioncogenes directly or indirectly. Correspondingly, multifarious 3-substituted indolin-2-one derivatives as selective kinase inhibitors for cancer therapy exhibited a low nanomolar activity with prominent efficacy, superior response rate and admirable tolerability. Particularly, certain 3-substituted indolin- 2-one derivatives have met the requirements for clinical trials or the pharmaceutical market. Herein, we focus on the traits of 3-substituted indolin-2-one derivatives as kinase inhibitors for cancer therapy, overview recent progress of 3-substituted indolin-2-one derivatives as kinase inhibitors for cancer therapy, analyze the selectivity for tyrosine kinases inhibitors and serine/threonine kinases inhibitors from the molecular aspects based on the molecular docking studies, summarize the structure-activity relationships (SARs) as selective kinase inhibitors and provide our perspectives for the development of 3- substituted indolin-2-one derivatives as kinase inhibitors for cancer therapy.

中文翻译：

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开发 3-取代的 Indolin-2-one 衍生物作为癌症治疗的激酶抑制剂。

激酶通过直接或间接调节癌基因的表达和抗癌基因的转录，是肿瘤发生和转移的关键调节剂。相应地，多种 3-取代的 indolin-2-one 衍生物作为癌症治疗的选择性激酶抑制剂表现出低纳摩尔活性，具有显着的疗效、优异的反应率和令人钦佩的耐受性。特别是某些3-取代二氢吲哚-2-酮衍生物已满足临床试验或药品市场的要求。在此，我们重点介绍了 3-取代 indolin-2-one 衍生物作为癌症治疗激酶抑制剂的特性，概述了 3-取代 indolin-2-one 衍生物作为癌症治疗激酶抑制剂的最新进展，