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Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
α-Glucosidase inhibitory derivatives of protocetraric acid
Huu-Hung Nguyen1, Thuc-Huy Duong2, Tran-Van-Anh Nguyen3
1Faculty of Applied Technology, School of Engineering and Technology, Van Lang University, Ho Chi Minh City, Vietnam.
Abstract:
Lichen-derived depsidones have been a successful source for alpha-glucosidase inhibitory agents with numerous advantages. In this article, derivatives of protocetraric acids were designed and synthesised. Diels-Alder reaction, esterification, and Friedel-Crafts alkylation of protocetraric acid with different reagents under Lewis acid were performed. Eleven products were prepared, including 10 new compounds and parmosidone A. Among them, compounds 2-4 and 6 had the novel skeletons. The newly synthetic products were evaluated for alpha-glucosidase inhibition. Among tested compounds, 9 showed the strongest activity, with an IC50 value of 5.9 µM. The molecular docking model indicated the consistency between in vitro and in silico data of alpha-glucosidase inhibition.
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