76104-21-7Relevant academic research and scientific papers
3,4-Disubstituted isothiazoles: Novel potent inhibitors of VEGF receptors 1 and 2
Kiselyov, Alexander S.,Semenova, Marina,Semenov, Victor V.
scheme or table, p. 1195 - 1198 (2009/08/07)
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-1. Active molecules also showed high intrinsic permeability (>30 × 10-5 cm/min) across Caco-2 cell monolayer.
