Benzamide and Benzamidine Compounds as New Inhibitors of Urokinasetype Plasminogen Activators

Mini Rev Med Chem. 2018;18(20):1753-1758. doi: 10.2174/1389557518666180816110740.

Abstract

Background & method: In this ongoing research, it is aimed to investigate the synthesis, structure identification and effects on urokinase-type plasminogen activators (uPA) and its receptor levels of 4-(3H-imidazo[4,5-b]pyridin-2-yl)-N-substituted benzamide and benzamidine derivatives. uPA levels obtained from 4b and 7d administration were similar to 5-FU (5-fluorouracil) for colorectal carcinoma cells (p<0.05). 4b and 7d significantly reduced uPAR (urokinase-type plasminogen activator receptor) levels on both cell lines (p<0.05).

Conclusion: uPAR levels obtaining from 4b and 7d administration were similar to 5-FU for both cell lines colorectal (Colo205, CCL-222) and hepatocellular (HepG2, CCL-23) carcinoma cells (p<0.05).

Keywords: Imidazopyridine; benzamide; benzamidine; uPAR; upamostat; urinary plasminogen activator..

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Benzamides / chemistry*
  • Benzamides / metabolism
  • Benzamides / pharmacology
  • Benzamidines / chemistry*
  • Benzamidines / metabolism
  • Benzamidines / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Receptors, Urokinase Plasminogen Activator / metabolism
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors
  • Urokinase-Type Plasminogen Activator / metabolism*

Substances

  • Antineoplastic Agents
  • Benzamides
  • Benzamidines
  • Enzyme Inhibitors
  • Receptors, Urokinase Plasminogen Activator
  • Urokinase-Type Plasminogen Activator