Noncyclam Tetraamines Inhibit CXC Chemokine Receptor Type 4 and Target Glioma-Initiating Cells

L Ros-Blanco, J Anido, R Bosser, J Esté…

Index: Ros-Blanco, Laia; Teixido, Jordi; Borrell, Jose I.; Anido, Judit; Seoane, Joan; Bosser, Ramon; Kosoy, Ana; Ruiz-Avila, Luis; Este, Jose; Clotet, Bonaventura Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7560 - 7570,11 Title/Abstract Full Text Show Details Ros-Blanco, Laia; Anido, Judit; Bosser, Ramon; Este, Jose; Clotet, Bonaventura; Kosoy, Ana; Ruiz-Avila, Luis; Teixido, Jordi; Seoane, Joan; Borrell, Jose I. Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7560 - 7570

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Citation Number: 3

Abstract

The three stereoisomers of the noncyclam compound 1 (1 (R, R), 1 (S, S), and the meso form 1 (S, R)) and their corresponding tetrahydrochlorides 11 were prepared from (S)-and (R)-2- methylpiperidine. We have evaluated their inhibitory activity on the CXC chemokine receptor type 4 (CXCR4), toxicity properties, and assessment of their effect on glioma initiating cells (GICs) in comparison with the prototype compound AMD3100. The IC50 values ...