Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368870 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
STATs are transcription factors acting as intracellular signaling after stimulation with cytokines, growth factors and hormones. STAT5 is also constitutively active in many forms of cancers, including chronic myelogenous leukemia, acute lymphoblastic leukemia and Hodgkin’s lymphoma. Recently, literature reported that the neuroleptic drug pimozide inhibits STAT5 phosphorylation inducing apoptosis in CML cells. We undertook an investigation from pimozide structure, obtaining simple derivatives with cytotoxic and STAT5-inhibitory activity, two of them markedly more potent than pimozide.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Riccardo Rondanin, Daniele Simoni, Romeo Romagnoli, Riccardo Baruchello, Paolo Marchetti, Cristiana Costantini, Sara Fochi, Giacomo Padroni, Stefania Grimaudo, Rosaria Maria Pipitone, Maria Meli, Manlio Tolomeo,