1194235-07-8

Basic information

• Product Name: (S)-methyl 3-(naphthalen-2-yl)-2-((S)-3-phenyl-2-(pyrazine-2-carboxamido)-propanamido) propanoate
• Synonyms: (S)-methyl 3-(naphthalen-2-yl)-2-((S)-3-phenyl-2-(pyrazine-2-carboxamido)-propanamido) propanoate
• CAS NO: 1194235-07-8
• Molecular Weight: 482.539
• Mol File: 1194235-07-8.mol
• Article Data: 4

Chemical Properties

• CAS DataBase Reference: (S)-methyl 3-(naphthalen-2-yl)-2-((S)-3-phenyl-2-(pyrazine-2-carboxamido)-propanamido) propanoate(CAS DataBase Reference)
• NIST Chemistry Reference: (S)-methyl 3-(naphthalen-2-yl)-2-((S)-3-phenyl-2-(pyrazine-2-carboxamido)-propanamido) propanoate(1194235-07-8)
• EPA Substance Registry System: (S)-methyl 3-(naphthalen-2-yl)-2-((S)-3-phenyl-2-(pyrazine-2-carboxamido)-propanamido) propanoate(1194235-07-8)

Safety Data

• Hazardous Substances Data: 1194235-07-8(Hazardous Substances Data)

Upstream product

• 63024-26-0 methyl (S)-2-amino-3-(naphthalen-2-yl)propanoate hydrochloride 
• 114457-94-2 (S)-3-phenyl-2[(pyrazine-2-carbonyl)-amino]propionic acid 
• 7524-50-7 methyl (2S)-2-amino-3-phenylpropanoate hydrochloride 
• 73058-37-4 N-(2-pyrazinylcarbonyl)-L-phenylalanine methyl ester 
• 98-97-5 2-pyrazylcarboxylic acid 

Downstream Products

• 1194235-21-6 N-(2-pyrazinecarbonyl)-L-phenylalanine-L-(2-naphthyl)-alanine 

Relevant articles and documents

Synthesis and biological activity of peptide proline-boronic acids as proteasome inhibitors

On the basis of the application of proline-boronic acid as pharmacophore in the kinase inhibitors and our previous research results, using proline-boronic acid as warhead, two series of peptide proline-boronic acids, dipeptide proline-boronic acids (I) and tripeptide proline-boronic acids (II), were designed and synthesized. All the synthesized compounds were first evaluated for their biological activity against MGC803 cell, and then, the best compound II-7 was selected to test its anti-tumor spectrum on six human tumor cell lines and proteasome inhibition against three subunits. The results indicated that series II have much better biological activities than series I. The compound II-7 exhibited not only excellent biological activities with IC50 values of nM level in both cell and proteasome models, but also much better subunit selectivity. Thus, proline-boronic acid as warhead is reasonable in the design of proteasome inhibitors.

TRIPEPTIDE BORONIC ACID OR BORONIC ESTER, PREPARATIVE METHOD AND USE THEREOF

The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.