3-Arylidene-N-hydroxyoxindoles: A New Class of Compounds Endowed with Antitumor Activity

Loana Musso, Raffaella Cincinelli, Valentina Zuco, Michelandrea De Cesare, Franco Zunino, Anna Lucia Fallacara, Maurizio Botta, Sabrina Dallavalle

Research output: Contribution to journalArticle

Abstract

A series of compounds containing the N-hydroxyoxindole scaffold were synthesized and evaluated for antitumor activity. The compounds showed potent antiproliferative activity against the wild-type p53 IGROV-1 ovarian carcinoma cell line and considerably lower efficacy against the mutant IGROV-1/Pt1 subline that lacks p53 function. The differential response of ovarian carcinoma cells depending on p53 status was also reflected in the varied susceptibility to apoptosis of the treated cell lines. These results support a role for the p53 transcription factor as a determinant of cytotoxicity. The therapeutic potential of the most promising compound of the series was evaluated in the treatment of an IGROV-1 xenograft growing as ascitic tumor in mice. Using intraperitoneal administration, daily treatment with the compound for four weeks produced a significant delay in the onset of ascites.

Original languageEnglish
Pages (from-to)1700-1704
Number of pages5
JournalChemMedChem
DOIs
Publication statusPublished - Aug 19 2016

Keywords

  • antiproliferative activity
  • antitumor agents
  • apoptosis
  • N-hydroxyoxindole
  • p53

ASJC Scopus subject areas

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

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  • Cite this

    Musso, L., Cincinelli, R., Zuco, V., De Cesare, M., Zunino, F., Fallacara, A. L., Botta, M., & Dallavalle, S. (2016). 3-Arylidene-N-hydroxyoxindoles: A New Class of Compounds Endowed with Antitumor Activity. ChemMedChem, 1700-1704. https://doi.org/10.1002/cmdc.201600225