title: Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors.
abstract: Selective inhibition of the transporter protein sodium-glucose cotransporter 2 (SGLT2) has emerged as a promising way to control blood glucose level in diabetes patients. Reported herein is a short and convergent synthetic route towards some small-molecule SGLT2 inhibitors by a chemo- and diastereospecific palladium-catalyzed arylation reaction. This synthetic strategy enabled the discovery of two highly selective and potent SGLT2 inhibitors, thereby paving the way towards the development of carbasugar SGLT2 inhibitors as potential antidiabetic/antitumor agents.
authors.affiliation: Department of Chemistry, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China.|Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts, 02139, USA.
authors.forename: Wai-Lung
authors.identifier: 0000-0003-2892-6318
authors.initials: WL
authors.lastname: Ng
authors.affiliation: Institute of Chinese Medicine and State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China.
authors.forename: Kit-Man
authors.initials: KM
authors.lastname: Lau
authors.affiliation: Institute of Chinese Medicine and State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China.
authors.forename: Clara B-S
authors.initials: CB
authors.lastname: Lau
authors.affiliation: Department of Chemistry, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China. tonyshing@cuhk.edu.hk.
authors.forename: Tony K M
authors.initials: TK
authors.lastname: Shing
keywords: carbohydrates; cross-coupling; drug design; inhibitors; palladium