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

作者：Rizvi Syed Umar Farooq; Siddiqui Hamid Latif^*; Nisar Muhammad; Khan Nematullah; Khan Inamullah

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(2): 942-944.

DOI：10.1016/j.bmcl.2011.12.017

• Quinolyl-thienyl chalcones
• Angiogenesis
• VEGFR-2 kinase
• Docking

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.

• 出版日期2012-1-15