Gao, Yongzhi; van Haren, Matthijs J.; Moret, Ed E.; Rood, Johannes J. M.; Sartini, Davide; Salvucci, Alessia; Emanuelli, Monica; Craveur, Pierrick; Babault, Nicolas; Jin, Jian; Martin, Nathaniel I. published an article in Journal of Medicinal Chemistry. The title of the article was 《Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT) with Enhanced Activity》.Product Details of 1877-71-0 The author mentioned the following in the article:
Nicotinamide N-methyltransferase (NNMT) catalyzes the methylation of nicotinamide to form N-methylnicotinamide. Overexpression of NNMT is associated with a variety of diseases, including a number of cancers and metabolic disorders, suggesting a role for NNMT as a potential therapeutic target. By structural modification of a lead NNMT inhibitor previously developed in our group, we prepared a diverse library of inhibitors to probe the different regions of the enzyme’s active site. This investigation revealed that incorporation of a naphthalene moiety, intended to bind the hydrophobic nicotinamide binding pocket via π-π stacking interactions, significantly increases the activity of bisubstrate-like NNMT inhibitors (half-maximal inhibitory concentration 1.41 μM). These findings are further supported by isothermal titration calorimetry binding assays as well as modeling studies. The most active NNMT inhibitor identified in the present study demonstrated a dose-dependent inhibitory effect on the cell proliferation of the HSC-2 human oral cancer cell line. The results came from multiple reactions, including the reaction of 3-(Methoxycarbonyl)benzoic acid(cas: 1877-71-0Product Details of 1877-71-0)
3-(Methoxycarbonyl)benzoic acid(cas: 1877-71-0) belongs to esters. Esters are more polar than ethers but less polar than alcohols. Product Details of 1877-71-0 They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics