page_title: VEGFR-2 inhibitor
section_title: Quinoline and quinazoline-derivatives
hierarchical_section_title: VEGFR-2 inhibitor / Structure-activity relationship (SAR) / Quinoline and quinazoline-derivatives
caption_attribution_description: English: Quinazoline structure
context_page_description: VEGFR-2 inhibitor, also known as kinase insert domain receptor inhibitor, are tyrosine kinase receptor inhibitors that reduce angiogenesis or lymphangiogenesis, leading to anticancer activity. Generally they are small, synthesised molecules that bind competitively to the ATP-site of the tyrosine kinase domain. VEGFR-2 selective inhibitor can interrupt multiple signaling pathways involved in tumor, including proliferation, metastasis and angiogenesis.
context_section_description: Lenvatinib, Vandetanib and Cabozantinib are drugs that belong to this group.
  Novel biphenyl tricyclic quinazoline compounds and aryloxy quinolone derivatives are multiple kinase inhibitors. They are less likely to lead to drug resistance than selective inhibitors, which increases life expectancy.
  4-quinazolinamine heterocyclic compounds and 2-chloro-4-anilino-quinazoline derivatives inhibit tumor vessel generation and restrain EGFR, HER-2, VEGFR-2 and mitosis process.Quinoxaline derivatives with a diaryl-amide or diaryl-urea substructure have B-Raf mutant kinase inhibition activity.
  Some novel quinazoline derivatives inhibit Raf kinase selectively and have less effect on inhibition of VEGFR-2 and EGFR kinase.
  A scaffold in position N1 on quinolone and quinazoline derivatives behaves as a hydrogen bond receptor and interacts with Cys919 residue. The terminal substituent aromatic ring can form hydrophobic bonds with the hydrophobic pocket of VEGFR-2, especially the terminal phenyl group substituted by chloride in the para-position.
  Quinolone-urea containing VEGFR inhibitors will bind to Asp1046 residue of the receptor via the carbonyl oxygen, and interact with Glu885 residue via two NH groups.
caption: Quinazoline structure
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