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6,7‐Dimethoxy‐Quinazolin‐4‐yl‐Amino‐Nicotinamide Derivatives as Potent Inhibitors of VEGF Receptor II
Author(s) -
Ashok Abhishek,
Thanukrishnan Kannan,
Bhojya Naik Halehatty S.,
Ghosh Soma
Publication year - 2017
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2750
Subject(s) - chemistry , angiogenesis , vegf receptors , vascular endothelial growth factor , nicotinamide , receptor , pharmacology , homogeneous , cancer research , enzyme , biochemistry , physics , thermodynamics , medicine , biology
The sprouting of new blood vessels, or angiogenesis, is necessary for any solid tumor to grow large enough to cause life‐threatening disease. Vascular endothelial growth factor (VEGF) is one of the key promoters of tumor‐induced angiogenesis. Inhibition of the VEGF signaling pathway has emerged as one of the most promising new approaches for cancer therapy . A series of 6,7‐dimethoxy‐quinazolin‐4‐yl‐amino‐nicotinamides were synthesized and evaluated as antagonists of VEGF receptor II (VEGFR‐2). Many compounds display VEGFR‐2 inhibitory activity, and compound 7a was found to be a potent inhibitor of VEGFR‐2 in an homogeneous time‐resolved fluorescence enzymatic assay with an IC 50 as low as 48 nM (comparable activity to ZD‐6474).