210832-85-2Relevant articles and documents
TGF-betaR1 inhibitor and application thereof
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Paragraph 0664; 0666-0668, (2020/06/09)
The invention belongs to the field of medical chemistry, and particularly relates to a compound serving as a TGF-betaR1 inhibitor and application of the compound. Specifically, the invention providesa compound shown as a formula I or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the compounds or the composition to treatment and/or prevention of TGF-betaR1 related diseases, such as cancers, tissue hyperplasia diseases, fibrosis and inflammatory diseases. The compound provided by the invention shows significant inhibitory activity on TGF-betaR1 kinase, and is very expected to become a therapeutic agent for TGF-betaR1 related diseases.
Photo- and PH-switchable fluorescent diarylethenes based on 2,3-diarylcyclopent-2-en-1-ones with dialkylamino groups
Shirinian, Valerii Z.,Lonshakov, Dmitry V.,Lvov, Andrey G.,Kavun, Alexey M.,Yadykov, Anton V.,Krayushkin, Mikhail M.
, p. 258 - 267 (2015/10/28)
New dialkylamino groups-comprising diarylethenes of 2,3-diarylcyclopent-2-en-1-one (DCP) series have been synthesized and its photochromic, fluorescent as well as acidochromic features have been investigated. It was shown that photochromic properties of t
Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: Clues for specific design of new compounds
Perez, Daniel I.,Palomo, Valle,Pérez, Concepción,Gil, Carmen,Dans, Pablo D.,Luque, F. Javier,Conde, Santiago,Martínez, Ana
experimental part, p. 4042 - 4056 (2011/08/05)
Development of kinase-targeted therapies for central nervous system (CNS) diseases is a great challenge. Glycogen synthase kinase 3 (GSK-3) offers a great potential for severe CNS unmet diseases, being one of the inhibitors on clinical trials for different tauopathies. Following our hypothesis based on the enhanced reactivity of residue Cys199 in the binding site of GSK-3, we examine here the suitability of phenylhalomethylketones as irreversible inhibitors. Our data confirm that the halomethylketone unit is essential for the inhibitory activity. Moreover, addition of the halomethylketone moiety to reversible inhibitors turned them into irreversible inhibitors with IC50 values in the nanomolar range. Overall, the results point out that these compounds might be useful pharmacological tools to explore physiological and pathological processes related to signaling pathways regulated by GSK-3 opening new avenues for the discovery of novel GSK-3 inhibitors.