660847-71-2

Upstream product

• 58521-45-2 tert-butoxycarbonyl-L-leucinal 
• 825-56-9 2-phenyl-1,3,4-oxadiazole 
• 660847-58-5 (1-{1(R/S)-[hydroxy-(5-phenyl-[1,3,4]oxadiazol-2-yl)-(S)-methyl]-3-methylbutylcarbamoyl}-2-(S)-methoxyethyl)carbamic acid tert-butyl ester 
• 890660-33-0 Boc-neopentyl-Asn-O-tBu 
• 660847-45-0 {1-[(R/S)-hydroxy-(5-phenyl-[1,3,4]oxadiazol-2-yl)-(S)-methyl]-3-methylbutyl}carbamic acid tert-butyl ester 
• 890660-09-0 (S)-2-(4-methylphenylsulfonamido)-4-(neopentylamino)-4-oxobutanoic acid 
• 5813-64-9 2.2-dimethylpropylamine 

Relevant academic research and scientific papers

Optimization of subsite binding to the β5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: Syntheses and cellular properties of potent, selective proteasome inhibitors

Beginning with the peptide sequence Cbz-Ile-Glu(OtBu)-Ala-Leu found in PSI (3), a series of vinyl sulfones (VS) were synthesized for evaluation as inhibitors of the chymotrypsin-like activity of the 20S proteasome. Variations at the key P3 position confir

PROTEASOME INHIBITORS

The present invention is directed to compounds that are proteasome inhibitors, pharmaceutical composition comprising such compounds and methods of treating diseases mediated by unregulated proteasome activity.