Huang, Ke published the artcileSynthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment, SDS of cas: 32333-53-2, the publication is European Journal of Medicinal Chemistry (2019), 45-57, database is CAplus and MEDLINE.
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.
European Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, SDS of cas: 32333-53-2.
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