391888-89-4

Upstream product

• 169032-99-9 (2S,4S)-4-Chloro-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester 
• 176306-17-5 (2S,4R)-4-tritylsulfanylpyrrolidine-1,2-dicarboxylic acid 1-tert-butyl-2-methyl diester 
• 337307-10-5 (2S,4R)-2-Hydroxymethyl-4-tritylsulfanyl-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 391888-88-3 (2S,4R)-2-(2,4,5-trifluorobenzyloxymethyl)-4-tritylsulfanylpyrrolidine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 393792-62-6 (2S,4R)-2-(2,4,5-trifluorobenzyloxymethyl)-4-tritylsulfanylpyrrolidine-1-carboxylic acid 2-methoxycarbonylphenyl ester 
• 393792-74-0 (2S,4R)-2-(2,4,5-Trifluoro-benzyloxymethyl)-4-tritylsulfanyl-pyrrolidine-1-sulfonic acid benzylamide 
• 844476-70-6 (2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]dioxin-5-yl ester 
• 393789-23-6 (2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenyl ester 
• 844476-69-3 (2S,4R)-2-(2,4,5-trifluorobenzyloxymethyl)-4-tritylsulfanylpyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]dioxin-5-yl ester 
• 391889-21-7 (2S,4R)-5-propyl-2-[2-(2,4,5-trifluorobenzyloxymethyl)-4-tritylsulfanylpyrrolidin-1-yl]pyrimidine 

Relevant academic research and scientific papers

Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells

Endothelin-1 (ET-1) is mitogenic and/or antiapoptotic in human cancers, and antagonists to ET-1 receptors are under evaluation for cancer treatment. Inhibition of ET-1 activation by the endothelin-converting enzymes 1 a-d (ECE-1a-d; EC 3.4.24.71) represents another approach to block the ET-1 effect in cancer. To evaluate this potential, we synthesized and characterized a series of low nanomolar nonpeptidic thiol-containing ECE-1 inhibitors, and evaluated their effect, as well as the effect of inhibitors for the related metalloproteases neprilysin (NEP; EC 3.4.24.11) and angiotensin-converting enzyme (ACE; EC 3.4.15.1), on human glioblastoma cell growth. Only ECE-1 inhibitors inhibited DNA synthesis by human glioblastoma cells. Exogenous addition of ET-1 or bigET-1 to glioblastoma cells did not counterbalance the growth inhibition elicited by ECE-1 inhibitors, suggesting that ECE-1 inhibitors block the proliferation of human glioblastoma cells most likely via a mechanism not involving extracellular production of ET-1. This class of molecules may thus represent novel therapeutic agents for the potential treatment of human cancer.

Pyrrolidine derivatives

The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.

Pyrrolidine derivatives

The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.