2912-62-1Relevant 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 (2017/08/15)
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.
Kinetic resolution of α-bromophenylacetamides using quinine or Cinchona alkaloid salts
Marzorati, Liliana,Fejfar, Jose L.,Tormena, Claudio F.,Vitta, Claudio Di
experimental part, p. 748 - 753 (2012/09/05)
The kinetic resolution of racemic α-bromophenylacetamides 1 was achieved in the presence of benzenethiolate and Cinchona alkaloid salts as phase-transfer catalysts or benzenethiol and quinine, yielding (S)-enantioenriched α-sulfanylated products. The observed stereoselection was rationalized on the basis of the best fitting of 1 and the resolving agent in the ternary complexes.
4-hydroxy-3-quinolinecarboxamides with antiarthritic and analgesic activities
Clemence,Le Martret,Delevallee,Benzoni,Jouanen,Jouquey,Mouren,Deraedt
, p. 1453 - 1462 (2007/10/02)
A series of 4-hydroxy-3-quinolinecarboxamides has been synthesized and evaluated by the oral route as antiinflammatory agents in carrageenin-induced foot edema and adjuvant-induced arthritis and as analgesic agents in the acetic acid induced writhing test. Among the most active molecules, some have shown both analgesic and acute antiinflammatory activities. Others, such as compounds 24, 37, and 52, were only powerful peripherally acting analgesics. Compound 52, being active at 1 mg/kg (ED50), is the most potent compound in the series. Some analogues, substituted in the 2-position by an alcohol, ester, or amine function, displayed potent antiarthritic activity in the same range as that of piroxicam and were also active in acute tests of inflammation and nociception. They inhibited the activity of both cyclooxygenase and 5-lipoxygenase at micromolar concentrations. Compound 102 (RU 43526) showed potent antiarthritic activity (adjuvant-induced arthritis, ED50 = 0.7 mg/kg, po), and gastrointestinal tolerance (ED100 250 mg/kg, po) and thus it is presently undergoing an extensive pharmacological evaluation.
