title: Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors.
abstract: Protein tyrosine phosphatase 1B (PTP-1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Studies have shown that PTP-1B knockout mice showed increased insulin sensitivity in muscle and liver as well as resistance to obesity. A series of hydroxy benzofuran methyl ketones and their naturally mimicking dimers and linear and angular furanochalcones and flavones have been evaluated as PTP-1B inhibitors. Screened compounds displayed good inhibitory activity.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. agoel13@yahoo.com
authors.forename: Manish
authors.initials: M
authors.lastname: Dixit
authors.forename: Brajendra K
authors.initials: BK
authors.lastname: Tripathi
authors.forename: Akhilesh K
authors.initials: AK
authors.lastname: Tamrakar
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
authors.forename: Brijesh
authors.initials: B
authors.lastname: Kumar
authors.forename: Atul
authors.initials: A
authors.lastname: Goel
mesh_terms: D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D003500:Cyclization; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D014638:Vanadates / Q000494:pharmacology
chemical_list: D001572:Benzofurans; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D014638:Vanadates; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases