Discovery of an Orally Efficacious MYC Inhibitor for Liver Cancer Using a GNMT-Based High-Throughput Screening System and Structure-Activity Relationship Analysis was written by Kant, Rajni;Yang, Ming-Hui;Tseng, Chih-Hua;Yen, Chia-Hung;Li, Wei-You;Tyan, Yu-Chang;Chen, Marcelo;Tzeng, Cherng-Chyi;Chen, Wei-Cheng;You, Kaiting;Wang, Wen-Chieh;Chen, Yeh-Long;Chen, Yi-Ming Arthur. And the article was included in Journal of Medicinal Chemistry in 2021.Quality Control of Ethyl 2-hydroxybenzoate This article mentions the following:
Glycine-N-Me transferase (GNMT) downregulation results in spontaneous hepatocellular carcinoma (HCC). Overexpression of GNMT inhibits the proliferation of liver cancer cell lines and prevents carcinogen-induced HCC, suggesting that GNMT induction is a potential approach for anti-HCC therapy. Herein, we used Huh7 GNMT promoter-driven screening to identify a GNMT inducer. Compound K78 was identified and validated for its induction of GNMT and inhibition of Huh7 cell growth. Subsequently, we employed structure-activity relationship anal. and found a potent GNMT inducer, K117. K117 inhibited Huh7 cell growth in vitro and xenograft in vivo. Oral administration of a dosage of K117 at 10 mpk (milligrams per kg) can inhibit Huh7 xenograft in a manner equivalent to the effect of sorafenib at a dosage of 25 mpk. A mechanistic study revealed that K117 is an MYC inhibitor. Ectopic expression of MYC using CMV promoter blocked K117-mediated MYC inhibition and GNMT induction. Overall, K117 is a potential lead compound for HCC- and MYC-dependent cancers. In the experiment, the researchers used many compounds, for example, Ethyl 2-hydroxybenzoate (cas: 118-61-6Quality Control of Ethyl 2-hydroxybenzoate).
Ethyl 2-hydroxybenzoate (cas: 118-61-6) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Quality Control of Ethyl 2-hydroxybenzoate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics