On June 27, 2019, Leung, Leo; Niculescu-Duvaz, Dan; Smithen, Deborah; Lopes, Filipa; Callens, Cedric; McLeary, Robert; Saturno, Grazia; Davies, Lawrence; Aljarah, Mohammed; Brown, Michael; Johnson, Louise; Zambon, Alfonso; Chambers, Tim; Menard, Delphine; Bayliss, Natasha; Knight, Ruth; Fish, Laura; Lawrence, Rae; Challinor, Mairi; Tang, HaoRan; Marais, Richard; Springer, Caroline published an article.Related Products of 98946-18-0 The title of the article was Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships. And the article contained the following:
Lysyl oxidase (LOX) is a secreted copper-dependent amine oxidase that cross-links collagens and elastin in the extracellular matrix and is a critical mediator of tumor growth and metastatic spread. LOX is a target for cancer therapy, and thus the search for therapeutic agents against LOX has been widely sought. We report herein the medicinal chem. discovery of a series of LOX inhibitors bearing an aminomethylenethiophene (AMT) scaffold. High-throughput screening provided the initial hits. Structure-activity relationship (SAR) studies led to the discovery of AMT inhibitors with sub-micromolar half-maximal inhibitory concentrations (IC50) in a LOX enzyme activity assay. Further SAR optimization yielded the orally bioavailable LOX inhibitor CCT365623 (I) with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Related Products of 98946-18-0
The Article related to aminomethylenethiophene derivative preparation structure activity relationship, anti metastatic inhibitor lysyl inhibitor aminomethylenethiophene compound, General Organic Chemistry: Synthetic Methods and other aspects.Related Products of 98946-18-0
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