The Development of 3-substituted Indolin-2-one Derivatives as Kinase Inhibitors for Cancer Therapy

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.

Automated summary

Kinases play a crucial role in tumorigenesis and metastasis by regulating the expression of oncogenes and antioncogenes. 3-substituted indolin-2-one derivatives have shown promising potential as selective kinase inhibitors for cancer therapy, with low nanomolar activity, high efficacy, and good tolerability.