Elgendy, Bahaa published the artcileSynthesis and structure activity relationship of the first class of LXR inverse agonists, HPLC of Formula: 1997-80-4, the publication is Bioorganic Chemistry (2022), 105540, database is CAplus and MEDLINE.
Liver X Receptors (LXRs) are members of the nuclear receptor family, and they play significant role in lipid and cholesterol metabolism Moreover, they are key regulators of several inflammatory pathways. Pharmacol. modulation of LXRs holds great potential in treatment of metabolic diseases, neurodegenerative diseases, and cancer. We were the first group to identify LXR inverse agonists SR9238 and SR9243 and demonstrate their potential utility in treating liver diseases and cancer. Here, we present the results of structure-activity relationship (SAR) studies, based around SR9238 and SR9243. This study led to identification of I, II, III and IV which were more potent inverse agonists than SR9238 and SR9243 and inhibited expression of the fatty acid synthase gene in DU145 cells. We previously demonstrated that inhibition of FASN is correlated to the anticancer activity of SR9243 and this suggests that new inverse agonists have great potential as anticancer agents. We identified compounds with distinct selectivity toward both LXR isoforms, which can be excellent tools to study the pharmacol. of both isoforms. We employed mol. dynamic (MD) simulations to better understand the mol. mechanism underlying inverse agonist activity and to guide our future design.
Bioorganic Chemistry published new progress about 1997-80-4. 1997-80-4 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,Benzene, name is 1-(2-Bromoethyl)-3-(trifluoromethyl)benzene, and the molecular formula is C9H8BrF3, HPLC of Formula: 1997-80-4.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary