376644-39-2

Upstream product

• 376644-37-0 (2R,3R,4S)-4-tert-Butoxycarbonylamino-3-hydroxy-5-phenyl-2-(3,4,5-trimethoxy-benzylamino)-pentanoic acid ethyl ester 
• 72155-45-4 Boc-L-phenylalaninal 
• 124818-94-6 ethyl (2E,4S)-4-[(tert-butoxycarbonyl)amino]-5-phenylpent-2-enoate 
• 376644-38-1 (2R,3R,4S)-4-tert-Butoxycarbonylamino-3-hydroxy-5-phenyl-2-(3,4,5-trimethoxy-benzylamino)-pentanoic acid 
• 66605-57-0 (S)-N-tert-butoxycarbonyl-2-amino-3-phenylpropanol 

Downstream Products

• 376644-13-2 {(S)-1-[(1S,2R,3R)-1-Benzyl-2-hydroxy-3-[(S)-1-(2-hydroxy-4-methoxy-benzylcarbamoyl)-2-methyl-propylcarbamoyl]-3-(3,4,5-trimethoxy-benzylamino)-propylcarbamoyl]-2,2-dimethyl-propyl}-carbamic acid tert-butyl ester 
• 376644-57-4 (2R,3R,4S)-4-((S)-2-Amino-3,3-dimethyl-butyrylamino)-3-hydroxy-5-phenyl-2-(3,4,5-trimethoxy-benzylamino)-pentanoic acid [(S)-1-(2-hydroxy-4-methoxy-benzylcarbamoyl)-2-methyl-propyl]-amide 
• 376644-36-9 (2R,3R,4S)-4-Amino-3-hydroxy-5-phenyl-2-(3,4,5-trimethoxy-benzylamino)-pentanoic acid [(S)-1-(2-hydroxy-4-methoxy-benzylcarbamoyl)-2-methyl-propyl]-amide 

Relevant academic research and scientific papers

Structure-based optimisation of 2-aminobenzylstatine derivatives: Potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome

We have identified 2-aminobenzylstatine derivatives that inhibit non-covalently the chymotrypsin-like activity of the human 20S proteasome. A structure-based optimisation approach has allowed us to improve the potency of this structural class of proteasome inhibitors from micromolar to nanomolar level. The new derivatives showed good selectivity against the trypsin-like and post-glutamyl-peptide hydrolytic activities of this enzyme.