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

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Massey AP, Harley WR, Pasupuleti N, Gorin FA, Nantz MH

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

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

PubMed ID

22366654 [ View in PubMed

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Abstract

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 muM and were cytotoxic to human U87 malignant glioma cells.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Amiloride	Urokinase-type plasminogen activator	IC 50 (nM)	7000	N/A	N/A	Details