Abstract

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.

Keywords: 3-Substituted indolin-2-one, kinase inhibitor, structure-activity relationship, cancer therapy, malignancy, ATP binding.