863036-33-3Relevant academic research and scientific papers
TARGETING OF ENDOPLASMIC RETICULUM DYSFUNCTION AND PROTEIN FOLDING STRESS TO TREAT NEUROLOGICAL CONDITIONS
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, (2019/10/15)
Methods and therapeutic compositions are disclosed for treating neurological disorders, such as Amyotrophic Lateral Sclerosis (ALS), Alzheimer's disease, Parkinson's disease and/or Huntington's disease, using Salubrinal analogs, or pharmaceutically acceptable salts, hydrates, or solvates thereof.
SAR, cardiac myocytes protection activity and 3D-QSAR studies of salubrinal and its potent derivatives
Liu,He,Li,Li,Liu,Zhong,Li
, p. 6072 - 6079 (2013/02/22)
Salubrinal is a selective inhibitor of endoplasmic reticulum (ER) stress and affords remarkable protection to cardiomyocytes. By studying the structure-activity relationship (SAR) of salubrinal, it was found that modification of the quinoline ring terminus and thiourea unit could confer the compound PP1-24 with markedly enhanced cardioprotective activity (EC 50 2 = 0.741, r2 = 0.991).
Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative
Long, Kai,Boyce, Michael,Lin, He,Yuan, Junying,Ma, Dawei
, p. 3849 - 3852 (2007/10/03)
The synthesis and structure-activity relationships (SAR) of salubrinal, a small molecule that protects cells from apoptosis induced by endoplasmic reticulum (ER) stress, are described. It is revealed that the trichloromethyl group greatly contributes to the activity. Based on the SAR results, salubrinal was converted into a biotinylated derivative which retains activity and can be used as a biological tool for target identification.
