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 in-dolin-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 kinas-es 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.
Original language | English (US) |
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Pages (from-to) | 1891-1919 |
Number of pages | 29 |
Journal | Current Medicinal Chemistry |
Volume | 29 |
Issue number | 11 |
DOIs | |
State | Published - Apr 2022 |
Keywords
- 3-Substituted indolin-2-one
- ATP binding
- cancer therapy
- kinase inhibitor
- malignan-cy
- structure-activity relationship
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Pharmacology
- Drug Discovery
- Organic Chemistry