140410-03-3

Upstream product

• 3113-72-2 5-methyl-2-nitrobenzoic acid 
• 40545-33-3 2-amino-5-methylbenzamide 
• 4315-12-2 5-methyl-2-nitrobenzamide 
• 91532-23-9 methyl-6-3H-benzotriazine-1,2,3 one-4 
• 86555-46-6 dimethyl (2S)-2-benzoylaminopentanedioate 

Downstream Products

• 140410-01-1 N-<4-<<(3,4-dihydro-4-oxo-1,2,3-benzotriazin-6-yl)methyl>amino>benzoyl>-L-glutamic acid 

Relevant academic research and scientific papers

N-amino>benzoyl>-L-glutamic Acid, a Novel A-Ring Analogue of 2-Desamino-5,8-dideazafolic Acid

N-amino>benzoyl>-L-glutamic acid ("2-aza-2-desamino-5,8-dideazafolic acid", ADDF) was synthesized from 2-amino-5-methylbenzamide via a four-step sequence consisting of diazotization, benzylic bromination, condensation with dimethyl N-(4-aminobenzoyl)-L-glutamate, and ester hydrolysis.ADDF was an inhibitor of recombinant mouse thymidylate synthase; inhibition was competitive with 5,10-methylenetetrahydrofolate as variable substrate (Ki=2.3μM).It was a substrate for murine folypolyglutamate synthetase with kinetic characteristics (Km=28μM) comparable to those of aminopterin, and it inhibited the growth of L1210 cells in culture (IC50=0.052μM).The structural modification of the A-ring embodied in ADDF appears to offer a novel, heterofore unexplored approach to the design of TS inhibitors.