80775-43-5Relevant academic research and scientific papers
Thienylhalomethylketones: Irreversible glycogen synthase kinase 3 inhibitors as useful pharmacological tools
Perez, Daniel I.,Conde, Santiago,Perez, Concepcion,Gil, Carmen,Simon, Diana,Wandosell, Francisco,Moreno, Francisco J.,Gelpi, Jose L.,Luque, Francisco J.,Martinez, Ana
experimental part, p. 6914 - 6925 (2010/02/28)
Thienylhalomethylketones, whose chemical, biological, and pharmaceutical data are here reported, are the first irreversible inhibitors of GSK-3β described to date. Their inhibitory activity is likely related to the cysteine residue present in the ATP-binding site, which is proposed as a relevant residue for modulation of GSK-3 activity. The good cell permeability of the compounds allows them to be used in different cell models. Overall, the results presented here support the potential use of halomethylketones as pharmacological tools for the study of GSK-3β functions and suggest a new mechanism for GSK-3β inhibition that may be considered for further drug design.
THIOPYRAN COMPOUNDS AS INHIBITORS OF MMP
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Page 49, (2010/02/05)
A compound of formula (I) in which R is lower alkyl, halogen, optionally substituted heterocyclic group or optionally substituted aryl, R is carboxy, protected carboxy or amidated carboxy, Ar is optionally substituted aryl or optionally substituted heterocyclic group, A is lower alkylene, X is oxa or a single bond, Y is thia, sulfinyl or sulfonyl, Z is methylene, thia, sulfinyl or sulfonyl, m and n are each an integer of 0 to 6, and 1/=m+n/=6, or its salt, which is useful as an inhibitor of matrix metalloproteinases (MMP) or tumor necrosis factor alpha (TNF alpha ).
Bromothiophene Reactions. I. Friedel-Crafts Acylation
Agua, M. J. del,Alvarez-Insua, A. S.,Conde, S.
, p. 1345 - 1347 (2007/10/02)
Friedel-Crafts acylation of 2,5-dibromo- and 2,3,5-tribromothiophenes with different acyl chlorides and anhydrous aluminium trichloride has been studied.The reaction afforded a mixture of acyl derivatives and tetrabromothiophene.The results obtained suggest a mechanism which involves the formation of bromine cations in the reaction medium.Several products obtained in this reaction are described.
