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

Zou, H, Zhang, L, Ouyang, J et al. (2011). Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents . EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 46(12), 5970-5977. 10.1016/j.ejmech.2011.10.009

cited authors

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

authors

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. © 2011 Elsevier Masson SAS. All rights reserved.

publication date

  • December 1, 2011

published in

Digital Object Identifier (DOI)

start page

  • 5970

end page

  • 5977

volume

  • 46

issue

  • 12