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Ng WL, Lau KM, Lau CB, et al. Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors. Angew Chem Int Ed Engl. 2016;55(44):13818-13821doi: 10.1002/anie.201608758.
Ng, W. L., Lau, K. M., Lau, C. B., & Shing, T. K. (2016). Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors. Angewandte Chemie (International ed. in English), 55(44), 13818-13821. https://doi.org/10.1002/anie.201608758
Ng, Wai-Lung, et al. "Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors." Angewandte Chemie (International ed. in English) vol. 55,44 (2016): 13818-13821. doi: https://doi.org/10.1002/anie.201608758
Ng WL, Lau KM, Lau CB, Shing TK. Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors. Angew Chem Int Ed Engl. 2016 Oct 24;55(44):13818-13821. doi: 10.1002/anie.201608758. Epub 2016 Oct 04. PMID: 27699962.
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Angew Chem Int Ed Engl. 2016 Oct 24;55(44):13818-13821. doi: 10.1002/anie.201608758. Epub 2016 Oct 04.

Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors.

Angewandte Chemie (International ed. in English)

Wai-Lung Ng, Kit-Man Lau, Clara B-S Lau, Tony K M Shing

Affiliations

  1. Department of Chemistry, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China.
  2. Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts, 02139, USA.
  3. 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.
  4. Department of Chemistry, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China. [email protected].

PMID: 27699962 DOI: 10.1002/anie.201608758

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.

© 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Keywords: carbohydrates; cross-coupling; drug design; inhibitors; palladium

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