Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents.

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Zou H, Zhang L, Ouyang J, Giulianotti MA, Yu Y

Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents.

Eur J Med Chem. 2011 Dec;46(12):5970-7. doi: 10.1016/j.ejmech.2011.10.009. Epub 2011 Oct 13.

PubMed ID

22019188 [ View in PubMed

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Abstract

Three series of 3-substituted-indolin-2-ones and azaindolin-2-ones have been synthesized and showed potential antiproliferative activity to cancer cell lines. The inhibition activities on VEGF-induced VEGFR phosphorylation were observed for selected 2-indolinones. Among the compounds synthesized, 5-fluoroindolin-2-one derivative 23 with a pyridone unit showed the most significant enzymatic and cellular activities. Flow cytometric analysis indicates that 23 plays a role in suppressing HCT-116 cell proliferation via G1 phase arrest and apoptosis in a dose dependent manner. The binding mode of compound 23 complexed with VEGFR-2 was predicted using FlexX algorithm. Described here are the chemistry and biological testing for these series which will guide the design and optimization of novel 2-indolione antitumor agents.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sunitinib	Vascular endothelial growth factor receptor 2	IC 50 (nM)	12	N/A	N/A	Details