关键词: 2-indolinone Inhibitor histone deacetylase mouse double minute 2 oxindole polo-like kinase tyrosine kinase inhibitors

Mesh : Animals Antineoplastic Agents / chemical synthesis chemistry pharmacology Chemistry, Pharmaceutical / methods Drug Design Humans Indoles / chemical synthesis chemistry pharmacology Molecular Targeted Therapy Neoplasms / drug therapy Oxindoles Patents as Topic

来  源:   DOI:10.1517/13543776.2016.1118059   PDF(Sci-hub)

Abstract:
BACKGROUND: 2-Indolinone is a well-known aromatic heterocyclic organic compound. A lot of work has been done on this bicyclic structure by academic and company researchers to synthesize compounds directed to a plethora of molecular targets in order to discover new drug leads. This review presents up-to-date information in the field of cancer therapy research based on this small building block.
METHODS: The present review gives an account of the recent patent literature (2008-2014) describing the discovery of 2-indolinone derivatives with selected therapeutic activities. In this period, a large amount of patents were published on this topic. We have limited the analysis to 37 patents on 2-indolinone derivatives having potential clinical application as chemotherapeutic agents. In this review, the therapeutic applications of 2-indolinone derivatives for the treatment of cancer reported in international patents have been discussed.
CONCLUSIONS: 2-Indolinone is the scaffold of the compounds considered from a medicinal chemistry perspective. Many of them have been developed and marketed for therapeutic use. In cancer chemotherapy, progress has been made in designing selective 2-indolinone derivatives. Some of them show preclinical efficacy. However, 2-indolinone has not exhausted all of its potential in the development of new compounds for clinical applications and remains a great tool for future research.
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