3, 4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2

AS Kiselyov, M Semenova, VV Semenov

文献索引：Kiselyov, Alexander S.; Semenova, Marina; Semenov, Victor V. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 4 p. 1195 - 1198

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被引用次数: 19

摘要

Novel derivatives of isothiazoles are described as potent ATP-competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR-1/2). A number of compounds exhibited VEGFR-2 inhibitory activity comparable to that of Vatalanib™ in both HTRF enzymatic and cellular assays. Several derivatives featuring bulky meta-substituents in the amide portion of the molecule displayed 4-to 8-fold specificity for VEGFR-2 versus VEGFR ...