INHIBITORS FOR THE Β-CATENIN / T-CELL FACTOR PROTEIN–PROTEIN INTERACTION
Disclosed are inhibitors for the β-catenin/T-cell factor interaction. The inhibitors are selective for β-catenin/T-cell factor over β-catenin/cadherin and β-catenin/APC interactions. Methods of using the disclosed compounds to treat cancer are also disclosed.
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Page/Page column 31; 35
(2019/10/23)
Acylation, cyanoethylation and alkylation of methyl and phenyl indolylmagnesium salts: Influence of the substituents on the C- and N- reaction products
Analysis of the influence of the substitution on indolylmagnesium salts in the reaction with benzoyl chloride, acrylonitrile and methyl iodide, giving the C- and N-derivatives, have been carried out. The yield in the C- and N-product depends upon the electronic character and position of the substituent (methyl or phenyl) on the indole ring and of the ethereal solvent as well as the concentration and molar ratio of the reagents. The 2- or 3- phenyl substituted indolylmagnesium salts with acrylonitrile always gave the 1-(2-cyanoethyl)indole derivative.
Rodriguez, J. Gonzalo,Urrutia, Anahi
p. 129 - 135
(2007/10/03)
Highly potent inhibitors of the Grb2-SH2 domain
Highly potent inhibitors of the Grb2-SH2 domain have been synthesized. They share the common sequence: Ac-Pmp-Ac6c-Asn-NH-(3-indolyl-propyl). Different substituents at the 3-indolyl-propylamine C-terminal group were explored to further improve the activity. This is the first example of inhibitors of SH2 domains with sub-nanomolar affinity reported to date.
Schoepfer, Joseph,Fretz, Heinz,Gay, Brigitte,Furet, Pascal,Garcia-Echeverria, Carlos,End, Nicole,Caravatti, Giorgio
p. 221 - 226
(2007/10/03)
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