1436405-75-2

Upstream product

• 1571-72-8 3-amino-4-hydroxybenzoic acid 
• 1201080-46-7 5-acetamido-4-ethoxy-2-nitrobenzoyl chloride 
• 1201080-29-6 5-acetamido-4-ethoxy-2-nitrobenzoic acid 
• 1356916-92-1 3-acetamido-4-ethoxybenzoic acid 
• 91004-38-5 3-acetamido-4-hydroxybenzoic acid 

Downstream Products

• 1436405-78-5 N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-4-ethoxy-5-(4-((4-methylpiperazin-1-yl)methyl)benzamido)-2-nitrobenzamide 
• 1436405-79-6 2-amino-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-4-ethoxy-5-(4-((4-methylpiperazin-1-yl)methyl)benzamido)benzamide 
• 1436405-76-3 N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-5-(4-(dimethylamino)but-2-enamido)-4-ethoxy-2-nitrobenzamide 
• 1436405-77-4 2-amino-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-5-(4-(dimethylamino)but-2-enamido)-4-ethoxybenzamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors

36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure-activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an IC50 value of 45 nM to EGFR kinase. Several compounds of other series also show IC50 values 1 μM for EGFR and 5 μM for A-549 and HL60 cells growth inhibition.