Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones

Eleonora Rizzi, Giuliana Cassinelli, Sabrina Dallavalle, Cinzia Lanzi, Raffaella Cincinelli, Raffaella Nannei, Giuditta Cuccuru, Franco Zunino

Research output: Contribution to journalArticlepeer-review

Abstract

A novel series of 3-arylureidobenzylidene-indolin-2-ones was synthesized and their inhibitory activity against Ret tyrosine kinase investigated in comparison with the Ret inhibitor RPI-1 as a reference compound for this series. A few compounds were able to revert the RETC634R oncogene-transformed morphologic phenotype of NIH3T3MEN2A cells and showed a selective antiproliferative activity against these cells as compared to parental NIH3T3 cells or NIH3T3 cells transformed with a non-tyrosine kinase oncogene (NIH3T3H-RAS). Inhibition of Ret enzyme activity by effective derivatives was confirmed in a kinase assay. Structure-activity relationship indicated a favourable activity for 5,6-dimethoxyindolinone derivatives with H, OH, or OMe in the para position of the distal aryl ring.

Original languageEnglish
Pages (from-to)3962-3968
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number14
DOIs
Publication statusPublished - Jul 15 2007

Keywords

  • Antitumour
  • Indolinone
  • Protein kinase
  • RET
  • Synthesis
  • Thyroid cancer

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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