1354558-41-0Relevant academic research and scientific papers
Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships
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,Ménard, Delphine,Bayliss, Natasha,Knight, Ruth,Fish, Laura,Lawrence, Rae,Challinor, Mairi,Tang, Haoran,Marais, Richard,Springer, Caroline
, p. 5863 - 5884 (2019/07/04)
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 chemistry 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 with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy.
Sulfonylation of five-membered heterocycles via an SNAr reaction
Liang, Shuai,Zhang, Ruo-Yi,Xi, Long-Yi,Chen, Shan-Yong,Yu, Xiao-Qi
, p. 11874 - 11880 (2014/01/06)
An efficient, concise, and transition metal-free synthesis of functionalized sulfonylated five-membered heterocyclic compounds via an S NAr reaction has been developed. Using commercially available sodium sulfinates as sulfonylation reagents, various five-membered heterocyclic sulfones were obtained in good yields.
A mild and efficient synthesis of aryl sulfones from aryl chlorides and sulfinic acid salts using microwave heating
Yuan, Yan-Qin,Guo, Sheng-Rong
supporting information; experimental part, p. 2750 - 2756 (2011/12/04)
The CuCl-catalyzed coupling of aryl chlorides and sulfinic acid salts provides a simple and extremely efficient route to unsymmetrical aryl sulfones in high to excellent yields under microwave irradiation within 3-30 minutes. Georg Thieme Verlag Stuttgart · New York.
