Synthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment was written by Huang, Ke;Jiang, Lulu;Liang, Ronghui;Li, Huiti;Ruan, Xiaoxue;Shan, Changliang;Ye, Deyong;Zhou, Lu. And the article was included in European Journal of Medicinal Chemistry in 2019.Related Products of 63624-28-2 This article mentions the following:
Phosphoglycerate mutase 1 (PGAM1) coordinates glycolysis, pentose phosphate pathway, and serine synthesis to promote tumor growth through the regulation of its substrate 3-phosphoglycerate (3 PG) and product 2-phosphoglycerate (2 PG). Herein, based on our previously reported PGAM1 inhibitor PGMI-004A, we have developed anthraquinone derivatives as novel allosteric PGAM1 inhibitors and the structure-activity relationship (SAR) was investigated. In addition, we determined the co-crystal structure of PGAM1 and the inhibitor 8g, demonstrating that the inhibitor was located at a novel allosteric site. Among the derivatives, compound 8t was selected for further study, with IC50 values of 0.25 and approx. 5 μM in enzymic and cell-based assays, resp. Mechanistically, compound 8t reduced the glycolysis and oxygen consumption rate in cancer cells, which led to decreased ATP (ATP) production and subsequent 5′ adenosine monophosphate-activated protein kinase (AMPK) activation. The inhibitor 8t also exhibited good efficacy in delaying tumor growth in H1299 xenograft model without obvious toxicity. Taken together, this proof-of-principle work further validates PGAM1 as a potential target for cancer therapy and provides useful information on anti-tumor drug discovery targeting PGAM1. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Related Products of 63624-28-2).
2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Related Products of 63624-28-2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics