858367-06-3

Upstream product

• 858366-90-2 (3S,4S)-3-Benzyloxy-4-methyl-1-nitro-hexan-2-ol 
• 66646-88-6 (E)-N-benzylideneglycine methyl ester 
• 100-52-7 benzaldehyde 
• 66646-88-6 methyl 2-(benzylideneamino)acetate 
• 56577-28-7 methyl (2S,3S)-2-hydroxy-3-methylpentanoate 
• 488-15-3 (2S,3S)-2-Hydroxy-3-methylpentanoic acid 
• 73-32-5 L-isoleucine 
• 858367-17-6 (2S,3R,4S,5S)-3-[(S)-1-(benzyloxy)-2-methybutyl]-2-methoxycarbonyl-4-nitro-5-phenylpyrrolidine 
• 858366-96-8 {[(E,3S,4S)-4-methyl-1-nitrohex-1-en-3-yloxy]methyl}benzene 
• 858366-75-3 methyl (2S,3S)-2-(benzyloxy)-3-methylpentanoate 
• 858366-85-5 (2S,3S)-2-Benzyloxy-3-methyl-pentan-1-ol 

Downstream Products

• 862666-28-2 {[(2S,3R,4S,5S)-3-((1S,2S)-1-Benzyloxy-2-methyl-butyl)-4-nitro-5-phenyl-pyrrolidine-2-carbonyl]-amino}-acetic acid methyl ester 
• 1420778-34-2 methyl {(2S,3R,4S,5S)-3-[(1S)-1-benzyloxy-2-methylbutyl]-4-nitro-5-phenyl}prolyl-β-alaninate 
• 1420778-36-4 methyl 4-{(2S,3R,4S,5S)-3-[(2S)-1-benzyloxy-2-methylbutyl]-4-nitro-5-phenyl-prolylamino}butanoate 
• 1420778-37-5 methyl 5-{(2S,3R,4S,5S)-3-[(2S)-1-benzyloxy-2-methylbutyl]-4-nitro-5-phenyl-prolylamino}pentanoate 
• 936712-88-8 methyl 6-{(2S,3R,4S,5S)-3-[(2S)-1-benzyloxy-2-methylbutyl]-4-nitro-5-phenyl-prolylamino}hexanoate 

Relevant academic research and scientific papers

Design, synthesis, and functional evaluation of leukocyte function associated antigen-1 antagonists in early and late stages of cancer development

The integrin leukocyte function associated antigen 1 (LFA-1) binds the intercellular adhesion molecule 1 (ICAM-1) by its αL-chain inserted domain (I-domain). This interaction plays a key role in cancer and other diseases. We report the structure-based design, small-scale synthesis, and biological activity evaluation of a novel family of LFA-1 antagonists. The design led to the synthesis of a family of highly substituted homochiral pyrrolidines with antiproliferative and antimetastatic activity in a murine model of colon carcinoma, as well as potent antiadhesive properties in several cancer cell lines in the low micromolar range. NMR analysis of their binding to the isolated I-domain shows that they bind to the I-domain allosteric site (IDAS), the binding site of other allosteric LFA-1 inhibitors. These results provide evidence of the potential therapeutic value of a new set of LFA-1 inhibitors, whose further development is facilitated by a synthetic strategy that is versatile and fully stereocontrolled.

Novel Inhibitors of the Lfa-1/Icam-1 Interaction and Uses Thereof

The invention relates to the treatment of disorders or diseases mediated by LFA-1/ICAM-1 molecular interaction. This is based on the use of novel chemical compounds capable of inhibiting said interaction, and more particularly, to pharmaceutical compositi

NOVEL INHIBITORS OF THE LFA-1/ICAM-1 INTERACTION, AND USES THEREOF

The invention relates to the treatment of disorders or diseases mediated by LFA-1/ ICAM-1 molecular interaction. This is based on the use of novel chemical compounds capable of inhibiting said interaction, and more particularly, to pharmaceutical composit

Novel synthetic compounds, processes of manufacture and uses in the treatment of integrin-mediated disorders

This invention relates to nitroproline derivative compounds and procedures for their preparation and the preparation of pharmaceutical compositions containing the compounds. The invention also relates to the administration of compounds of the invention as

Application of stereocontrolled stepwise [3+2] cycloadditions to the preparation of inhibitors of α4β1-integrin- mediated hepatic melanoma metastasis

(Chemical Equation Presented) Inhibitors of the interaction between protein VLA-4 and its natural ligand VCAM-1 have been designed, even though the structure of the protein remains unresolved. The rational design relied on the simulation of the steric and electronic properties of the active loop of VCAM-1, whose structure is known (see picture), and the inhibitors were readily prepared by stereoselective stepwise [3+2] cycloadditions.