130689-17-7Relevant articles and documents
A class of 2-benzylene tetrahydronaphthalone derivatives and preparation methods and applications thereof
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Paragraph 0188-0192; 0203-0208, (2022/03/31)
The present invention relates to the field of biotechnology, discloses a class of 2-benzylene tetrahydrophthalone derivatives and preparation methods and applications thereof. 2-Benzylene tetrahydronaphthalone derivative having the following structural formula, wherein R1 is selected from chlorine, bromine, iodine, alkyl, alkoxy, substituted or unsubstituted amino, alkylthio, alkyneoxy, hydroxy or hydroxymethyl group; R2, R3, R4 are hydrogen or carboxyl-containing substituents, and R2, R3, or R4 At least one of them is a carboxyl-containing substituent group. The present invention innovatively proposes a class of 2-benzylene tetrahydronaphthalone derivatives as a new skeleton of firefly luciferase inhibitors. A class of 2-benzylene tetrahydronaphthone derivatives of the present invention having a highly efficient inhibitor of nanomolar and a nanamol IC50; by competing with D- fluorescein reversibly inhibits firefly luciferase, and exhibits a high effect of firefly glowworm luciferase inhibition at the enzyme, intracellular and in vivo levels; at the same time, it is shown that it has good biocompatibility and application potential.