112918-77-1

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 83528-16-9 methyl 2-(4-aminophenyl)acetate hydrochloride 
• 39552-81-3 methyl p-aminophenylacetate 
• 117551-07-2 (4-Amino-phenyl)-acetyl chloride 
• 1197-55-3 4-aminophenylacetic acid 

Downstream Products

• 494224-44-1 [3-(4-tert-butoxycarbonylaminophenyl)-2-oxopropyl]phosphonic acid dimethyl ester 
• 695171-91-6 4-(tert-butyloxycarbonylamino)phenylacetaldehyde 
• 104060-23-3 tert-butyl N-[4-(2-hydroxyethyl)phenyl]carbamate 
• 135569-20-9 methyl 1-(p-aminophenyl)cyclopentanecarboxylate 
• 1275609-09-0 N-[4-(1-cyanocyclopentyl)phenyl][2-[(4-pyridylmethyl)amino](3-pyridyl)]carboxamide 

Relevant academic research and scientific papers

Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions

Nuclear factor erythroid 2-related factor 2 (NRF2) is a pleiotropic transcription factor which regulates the constitutive and inducible transcription of a wide array of genes and confers protection against a variety of pathologies. Directly disrupting Kelch-like ECH-associated protein 1 (KEAP1)-NRF2 protein-protein interaction (PPI) has been explored as a promising strategy to activate NRF2. We reported here the first identification of a series of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 inhibitors. Our efforts led to the potent small molecule KEAP1-NRF2 inhibitor, 20c, which exhibited a Kd of 24 nM to KEAP1 and an IC50 of 75 nM in disrupting KEAP1-NRF2 interaction. Subsequent biological studies provided consistent evidence across mouse macrophage cell-based and in vivo models that 20c induced NRF2 target gene expression and enhanced downstream antioxidant and anti-inflammatory activities. Our study not only demonstrated that small molecule KEAP1-NRF2 PPI inhibitors can be potential preventive and therapeutic agents for diseases and conditions involving oxidative stress and inflammation but also enriched the chemical diversity of the KEAP1-NRF2 inhibitors.

Synthesis and structure-activity relationships of phosphonic arginine mimetics as inhibitors of the M1 and M17 aminopeptidases from plasmodium falciparum

The malaria parasite Plasmodium falciparum employs two metallo- aminopeptidases, PfA-M1 and PfA-M17, which are essential for parasite survival. Compounds that inhibit the activity of either enzyme represent leads for the development of new antimalarial drugs. Here we report the synthesis and structure-activity relationships of a small library of phosphonic acid arginine mimetics that probe the S1 pocket of both enzymes and map the necessary interactions that would be important for a dual inhibitor.

PYRAZOLE DERIVATIVES AS INHIBITORS OF STAT3

Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles