391889-57-9

Upstream product

• 2646-90-4 2,5-difluorobenzaldehyde 
• 391889-56-8 (2S,4R)-[[1-(5-propylpyrimidin-2-yl)-4-tritylsulfanylpyrrolidin-2-yl]methyl]amine 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 391889-55-7 (2S,4R)-2-[1-(5-propylpyrimidin-2-yl)-4-tritylsulfanylpyrrolidin-2-ylmethyl]isoindole-1,3-dione 
• 391889-54-6 (2S,4R)-[1-(5-propylpyrimidin-2-yl)-4-tritylsulfanylpyrrolidin-2-yl]methanol 
• 391889-53-5 (2S,4R)-(4-tritylsulfanylpyrrolidin-2-yl)methanol 
• 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 

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.