期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 18, 页码 4568-4574出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.07.069
关键词
STAT5 inhibitors; Pimozide; BCR/ABL expressing leukemia; Apoptosis; Cell growth inhibition
资金
- Ministero dell'Universita e della Ricerca Scientifica e Tecnologica
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. (C) 2014 Elsevier Ltd. All rights reserved.
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