863036-65-1

Upstream product

• 863036-33-3 3-phenyl-N-(2,2,2-trichloro-1-isothiocyanato-ethyl)-acrylamide 
• 102-92-1 Cinnamoyl chloride 
• 140-10-3 (E)-3-phenylacrylic acid 
• 16535-67-4 (2E)-3-phenyl-N-[1-hydroxy-2,2,2-trichloroethyl]-2-acrylamide 
• 621-79-4 cinnamamide 

Downstream Products

• 1349043-29-3 (2E)-3-phenyl-N-[1-(8-quinolylamino)oxoformylamino-2,2,2-trichloroethyl]-2-acrylamide 
• 1349043-31-7 (2E)-3-phenyl-N-[1-(4-tolylamino)oxoformylamino-2,2,2-trichloroethyl]-2-acrylamide 
• 1429483-73-7 C₁₉H₁₈Cl₃N₃O₃ 
• 1429483-74-8 C₁₈H₁₅Cl₄N₃O₂ 
• 1429483-83-9 C₁₂H₉Cl₃N₂O₂ 

Relevant academic research and scientific papers

UREA COMPOUNDS AND USE THEREOF FOR INHIBITING APOPTOSIS

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof. The present invention also relates to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. Further, the present invention relates to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for anti-apoptosis, preventing or treating a disease or disorder associated with apoptosis; especially useful for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.

UREA COMPOUNDS AND USE THEREOF FOR INHIBITING APOPTOSIS

A compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, is provided. Also, a composition containing a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents, is provided. Further, use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof for anti-apoptosis is provided, preventing or treating a disease or disorder associated with apoptosis; especially for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.

SAR, cardiac myocytes protection activity and 3D-QSAR studies of salubrinal and its potent derivatives

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

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.