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1 H ‐1,2,4‐Triazol‐3‐yl‐anilines: Novel Potent Inhibitors of Vascular Endothelial Growth Factor Receptors 1 and 2
Author(s) -
Kiselyov Alexander S.,
Piatnitski Evgueni,
Milligan Daniel,
Ouyang Xiaohu
Publication year - 2007
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.1747-0285.2007.00507.x
Subject(s) - chemistry , receptor , vascular endothelial growth factor , vandetanib , enzyme , biochemistry , stereochemistry , biophysics , vegf receptors , pharmacology , biology , tyrosine kinase , cancer research
Novel derivatives of 1,2,4‐triazoles are described as potent ATP‐competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR‐1/2). A number of compounds display VEGFR‐2 inhibitory activity comparable to that of Vatalanib TM and Vandetanib TM in both homogenous time‐resolved fluorescence enzymatic and cellular assays. Several active molecules feature high intrinsic permeability (>30 × 10 −5 cm/min) across Caco‐2 cell monolayer.