Synthesis of 1-furfuryl-indolin-2-one derivatives and preliminary evaluation of their antitumor activities

Xiao Chun Dong, Fu Sheng Zhou, Jian Bin Zheng, Ren Wen*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


In order to find new indolin-2-one derivatives as antitumor agents, a series of 3-pyrrole substituted 1-(5-formyl-2-furanylmethyl) indolin-2-one derivatives were designed and synthesized. 5-Formyl-2,4-dimethyl-1II-pyrrole-3- carboxylic acid ethyl ester was condensed with 5-substituted indolin-2-one 2a -2d to afford 3-[(pyrrol-2-yl)-methylidenyl] indolin-2-ones 3a-3d. Through N-alkylation, 1-(5-formyl-furfuryl)-indolin-2-one 4a- 4d were prepared. Compounds 4a-4d were then condensed with indolin-2-one to afford bis-indolin-2-one derivatives 5a-5d. The structures of the synthesized compounds were determined by 1H NMR, MS and element analysis. Antitumor activities of all the synthesized compounds in vitro were tested. All the 12 synthesized compounds possess antitumor activities against SPC-A1 strain. Especially the compounds 5a-5d possess potent antitumor activities better than sunitinib. Their IC50 are all below 5 μmol · L -1.

Original languageEnglish (US)
Pages (from-to)54-59
Number of pages6
JournalYaoxue Xuebao
Issue number1
StatePublished - Jan 1 2008


  • Antitumor
  • Derivative
  • Indolin-2-one
  • Synthesis

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)


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