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Discovery and molecular docking of quinolyl-thienyl chalcones as anti-angiogenic agents targeting VEGFR-2 tyrosine kinase

  作者 Rizvi, SUF; Siddiqui, HL; Nisar, M; Khan, N; Khan, I  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-2;  页码  942-944  
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[摘要]Vascular endothelial growth factor Receptor-2 (VEGFR-2) kinase inhibition is one of the well established strategies to promptly tackle tumor growth by suppression of angiogenesis. In the current study, structure-based virtual screening methodology of a series of quinolyl-thienyl chalcones indicated their strong potential as VEGFR-2 kinase inhibitors. In vitro VEGFR-2 kinase inhibitory activity was found to be significant (compound 19, IC50: 73.41 nM). All compounds showed significant inhibition of human umbilical vein endothelial cells (HUVEC) proliferation (compound 19, IC50: 21.78 nM). Molecular interactions of the compounds were studied using molecular docking studies. (C) 2011 Elsevier Ltd. All rights reserved.

 
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