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.
Rondanin, R., Simoni, D., Romagnoli, R., Baruchello, R., Marchetti, P., Costantini, C., et al. (2014). Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 24(18), 4568-4574 [10.1016/j.bmcl.2014.07.069].
Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives
GRIMAUDO, Stefania;PIPITONE, Rosaria Maria;MELI, Maria;
2014-01-01
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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