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4‐(Azolylphenyl)‐phthalazin‐1‐amines: Novel Inhibitors of VEGF Receptors I and II
Author(s) -
Kiselyov Alexander S.,
Semenov Victor V.,
Milligan Daniel
Publication year - 2006
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2006.00456.x
Subject(s) - phthalazine , vegf receptors , chemistry , receptor , kinase insert domain receptor , selectivity , ic50 , pharmacology , vascular endothelial growth factor , enzyme , biochemistry , combinatorial chemistry , stereochemistry , vascular endothelial growth factor a , in vitro , biology , cancer research , medicinal chemistry , catalysis
Novel potent derivatives of phthalazine are described as ATP‐competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR‐1/2). A number of compounds display VEGFR‐2 inhibitory activity reaching that of Vatalanib TM 3 (IC 50 < 100 n m ) in an HTRF enzymatic assay. Several derivatives also show good potential for the development as VEGFR‐2 specific inhibitors showing 15–20‐fold selectivity over VEGFR‐1.