QSAR study on N-(aryl)-4-(azolylethyl) thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II

Med Chem. 2009 Sep;5(5):455-61. doi: 10.2174/157340609789117813. Epub 2009 Sep 1.

Abstract

QSAR study on N-(Aryl)-4-(azolylethyl) thiazole-5-carboxamides analogues, which are novel potent inhibitor of VEGF receptor II and I, were performed using topological, electronic and physicochemical descriptors. The results obtained demonstrate in detail, which specify that topological descriptors of the compounds play a significant role in developing QSAR models. The significance of presence and absence of substituents on particular position is successfully explored with the help of indicator variables. The results are critically discussed on the basis of multiple linear regression parameters.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry*
  • Amides / pharmacology*
  • Enzyme-Linked Immunosorbent Assay
  • Inhibitory Concentration 50
  • Quantitative Structure-Activity Relationship*
  • Thermodynamics
  • Vascular Endothelial Growth Factor Receptor-1 / antagonists & inhibitors*
  • Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*

Substances

  • Amides
  • Vascular Endothelial Growth Factor Receptor-1
  • Vascular Endothelial Growth Factor Receptor-2