Dokla, Eman M. E. published the artcileDevelopment of Potent Adenosine Monophosphate Activated Protein Kinase (AMPK) Activators, Product Details of C8H6BrF3S, the publication is ChemMedChem (2015), 10(11), 1915-1923, database is CAplus and MEDLINE.
Previously, the authors reported the identification of a thiazolidinedione-based adenosine monophosphate activated protein kinase (AMPK) activator, compound 1 (N-(4-((3-((1-methylcyclohexyl)methyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenyl)-4-nitro-3-(trifluoromethyl)benzenesulfonamide), which provided a proof of concept to delineate the intricate role of AMPK in regulating oncogenic signaling pathways associated with cell proliferation and epithelial-mesenchymal transition (EMT) in cancer cells. In this study, the authors used compound 1 as a scaffold to conduct lead optimization, which generated a series of derivatives Anal. of the antiproliferative and AMPK-activating activities of individual derivatives revealed a distinct structure-activity relationship and identified 59 (N-(3-nitrophenyl)-N’-(4-((3-((3,5-bis(trifluoromethyl)phenyl)methyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenyl)urea) as the optimal agent. Relative to 1, compound 59 exhibits multifold higher potency in upregulating AMPK phosphorylation in various cell lines irresp. of their liver kinase B1 (LKB1) functional status, accompanied by parallel changes in the phosphorylation/expression levels of p70S6K, Akt, Foxo3a, and EMT-associated markers. Consistent with its predicted activity against tumors with activated Akt status, orally administered 59 was efficacious in suppressing the growth of phosphatase and tensin homolog (PTEN)-null PC-3 xenograft tumors in nude mice. Together, these findings suggest that 59 has clin. value in therapeutic strategies for PTEN-neg. cancer and warrants continued investigation in this regard.
ChemMedChem published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Product Details of C8H6BrF3S.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary