title: Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors.
abstract: A series of bromo-retrochalcones was designed, synthesized and evaluated as PTP1B inhibitors based on licochalcone A and E. Compounds 6, 12, 13, 14, 25, 36, 37, 39, and 41 showed potent inhibitory effects against PTP1B, and compound 37, the most potent among the series, had an IC(50) value of 1.9 μM, about two-fold better than that of the positive control, ursolic acid.
authors.affiliation: College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Buk-Gu, Gwangju, Republic of Korea.
authors.forename: Zhiguo
authors.initials: Z
authors.lastname: Liu
authors.forename: Woojung
authors.initials: W
authors.lastname: Lee
authors.forename: Su-Nam
authors.initials: SN
authors.lastname: Kim
authors.forename: Goo
authors.initials: G
authors.lastname: Yoon
authors.forename: Seung Hoon
authors.initials: SH
authors.lastname: Cheon
mesh_terms: D001966:Bromine / Q000737:chemistry* / Q000494:pharmacology; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D047188:Chalcones; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; C070840:licochalcone A; D001966:Bromine