287474-36-6Relevant 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.
Heterocyclization of compounds containing diazo and cyano groups. 6. Theoretical and experimental investigations of cyclization of 2-cyano-2-diazoacetamides to 5-hydroxy-1,2,3-triazole-4-carbonitriles
Morzherin,Kolobov,Mokrushin,Brauer,Anders,Bakulev
, p. 22 - 36 (2007/10/03)
A series of N-alkyl- and N-aryl-2-cyano-2-diazoacetamides was synthesized by the reaction of 2-amino-2-cyanoacetamides with sodium nitrite in hydrochloric acid. The mechanism of their heteroelectrocyclization to 5-hydroxy-1,2,3-triazoles was investigated
