1486-48-2Relevant articles and documents
Mimic catechins to develop selective MMP-2 inhibitors
Di Pizio, Antonella,Agamennone, Mariangela,Laghezza, Antonio,Loiodice, Fulvio,Tortorella, Paolo
, p. 1293 - 1300 (2018)
Abstract: Matrix metalloproteinase 2 (MMP-2) is a well-known anticancer target belonging to the MMP family. Because of the bilateral role of MMPs in cancer, developing highly selective MMP-2 inhibitors is a current challenge. In this paper, we investigated the binding modes of green tea polyphenols epigallocatechin gallate and epicatechin into the active site of the MMP-2 enzyme. The structure-based analysis allowed the optimization of these hits and hence led to a better lead candidate. Moreover, using a pharmacophore model, we screened FooDB compounds and selected food components as potential MMP-2 inhibitors. The search for food-derived compounds that target this enzyme may represent a strategy to identify new lead molecules with improved safety profiles and provide indications about possible functional foods. Graphical abstract: [Figure not available: see fulltext.].
Promotion of mitochondrial biogenesis by synthetic 1,2- or 1,3-digallates through activation of an energy sensing network
Chong, Youhoon,Kim, Mi Kyoung,Lee, Taegum
, (2022/01/08)
Based on the observations suggesting that a digallate functionality might serve as a novel scaffold for inducers of mitochondrial biogenesis, we prepared a series of digallates and evaluated their activity in an in vitro model widely used in PD research (
Cannabidiol derivative, preparation method and application thereof
-
, (2021/07/28)
The invention discloses a cannabidiol derivative, a preparation method and application thereof, and belongs to the technical field of medicinal chemistry, wherein the cannabidiol derivative is obtained by taking cannabidiol as a main body through a synthesis means, and an anti-tumor activity determination result shows that the cannabidiol derivative prepared by the invention has an inhibition effect on lung cancer cell strains, human breast cancer cell strains, nasopharynx cancer and drug-resistant strains thereof.
Synthesis of B-ring-fluorinated (?)-epicatechin gallate derivatives
Baumgarten, Kai D.,Czekelius, Constantin,Michaelis, Carina S.,Thieltges, David D. S.
, p. 4024 - 4028 (2020/06/09)
The synthesis of enantiomerically pure B-ring fluorinated catechin derivatives is presented. In a convergent approach the chromane was obtained by reaction of a lithiated fluoro-resorcine with an optically active epoxide. The latter was prepared from 3,4-