556110-53-3Relevant 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
scheme or table, 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.
Compounds and their therapeutic use
-
, (2008/06/13)
Compounds of formula I: [wherein: X represents —CH═CH—, —CH═CR—, —CR═CR—, —CO—, —O—, —NH—, —NR—, S—, —SO—, —SO2—, —CH═N—, —CR═N—, —CH═N(O)—, —CR═N(O)— or any other atom or group of atoms capable of forming a S— or 6-membered heterocyclic ring;
Thienyl and Phenyl α-Halomethyl Ketones: New Inhibitors of Glycogen Synthase Kinase (GSK-3β) from a Library of Compound Searching
Conde, Santiago,Pérez, Daniel I.,Martínez, Ana,Perez, Concepción,Moreno, Francisco J.
, p. 4631 - 4633 (2007/10/03)
Glycogen synthase kinase (GSK-3β) plays a crucial role in Alzheimer's disease (AD). Its inhibition is a valid approach to the treatment of AD. In this initial letter, some thienyl and phenyl α-halomethyl ketones are described as new non-ATP competitive inhibitors of GSK-3β. They are considered as lead compounds for designing and synthesizing new series, to carry out SAR studies, clear up the mechanism of action, and, in general, evaluate their therapheutical usefulness.
