162045-53-6Relevant articles and documents
Effects of Pimozide Derivatives on pSTAT5 in K562 Cells
Rondanin, Riccardo,Simoni, Daniele,Maccesi, Martina,Romagnoli, Romeo,Grimaudo, Stefania,Pipitone, Rosaria Maria,Meli, Maria,Cascio, Antonio,Tolomeo, Manlio
, p. 1183 - 1190 (2017)
STAT5 is a transcription factor, a member of the STAT family of signaling proteins. STAT5 is involved in many types of cancer, including chronic myelogenous leukemia (CML), in which this protein is found constitutively activated as a consequence of BCR-ABL expression. The neuroleptic drug pimozide was recently reported to act as an inhibitor of STAT5 phosphorylation and is capable of inducing apoptosis in CML cells in vitro. Our research group has synthesized simple derivatives of pimozide with cytotoxic activity and that are able to decrease the levels of phosphorylated STAT5. In this work we continued the search for novel STAT5 inhibitors, synthesizing compounds in which the benzoimidazolinone ring of pimozide is either maintained or modified, in order to obtain further structure–activity relationship information for this class of STAT5 inhibitors. Two compounds of the series showed potent cytotoxic activity against BCR-ABL-positive and pSTAT5-overexpressing K562 cells and were able to markedly decrease the levels of phosphorylated STAT5.
Method for treating allergies using substituted pyrazoles
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, (2008/06/13)
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
Design and synthesis of N-alkylated saccharins as selective α-1a adrenergic receptor antagonists
Nerenberg, Jennie B.,Erb, Jill M.,Thompson, Wayne J.,Lee, Hee-Yoon,Guare, James P.,Munson, Peter M.,Bergman, Jeffrey M.,Huff, Joel R.,Broten, Theodore P.,Chang, Raymond S. L.,Chen, Tsing B.,O'Malley, Stacey,Schorn, Terry W.,Scott, Ann L.
, p. 2467 - 2472 (2007/10/03)
Benign prostatic hyperplasia can be managed pharmacologically with α-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the α-la receptor subtype may offer advantages in clinical applications with respect to hypotensive side effect