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Bioorg Med Chem Lett. 2012 Apr 1;22(7):2635-9. doi: 10.1016/j.bmcl.2011.12.123. Epub 2012 Jan 4.

2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.

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  • 1Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.


The relative non-toxicity of the diuretic amiloride, coupled with its selective inhibition of the protease urokinase plasminogen activator (uPA), makes this compound class attractive for structure-activity studies. Herein we substituted the C(2)-acylguanidine of C(5)-glycyl-amiloride with amidine and amidoxime groups. The data show the importance of maintaining C(5)-hydrophobicity. The C(5)-benzylglycine analogs containing either C(2)-acylguanidine or amidine inhibited uPA with an IC(50) ranging from 3 to 7 μM and were cytotoxic to human U87 malignant glioma cells.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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