Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cellswith new pimozide derivatives

Maria Meli, Rosaria Maria Pipitone, Stefania Grimaudo, Cristiana Costantini, Giacomo Padroni, Sara Fochi, Paolo Marchetti, Riccardo Baruchello, Riccardo Rondanin, Daniele Simoni, Romeo Romagnoli

Risultato della ricerca: Articlepeer review

18 Citazioni (Scopus)

Abstract

STATs are transcription factors acting as intracellular signaling after stimulation with cytokines, growthfactors and hormones. STAT5 is also constitutively active in many forms of cancers, including chronicmyelogenous leukemia, acute lymphoblastic leukemia and Hodgkin’s lymphoma. Recently, literaturereported that the neuroleptic drug pimozide inhibits STAT5 phosphorylation inducing apoptosis inCML cells. We undertook an investigation from pimozide structure, obtaining simple derivatives withcytotoxic and STAT5-inhibitory activity, two of them markedly more potent than pimozide.
Lingua originaleEnglish
pagine (da-a)4568-4574
Numero di pagine7
RivistaBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume24
Stato di pubblicazionePublished - 2014

All Science Journal Classification (ASJC) codes

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

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