500866-00-2Relevant articles and documents
Method for preparing 7, 8-dihydroxyflavone
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, (2022/04/08)
A method for preparing 7, 8-dihydroxyflavone relates to a preparation process of (3-pentylphenyl) acetic acid, and comprises the following steps: by taking pyrogallol as a raw material, carrying out Friedel-Crafts reaction with acetyl chloride to prepare 2, 3, 4-trihydroxyacetophenone, selectively protecting 3-and 4-hydroxyl groups by using benzyl chloride, carrying out esterification reaction on the unprotected 2-hydroxyl group and benzoyl chloride, and separating and purifying the 2, 3, 4-trihydroxyacetophenone to obtain 7, 8-dihydroxyflavone. And carrying out Baker-Venkatarman rearrangement, ring closing and debenzylation on an esterification product, so as to obtain the 8-dihydroxy flavone.
Studies on gambogic acid (IV): Exploring structure-activity relationship with IκB kinase-beta (IKKβ)
Sun, Haopeng,Chen, Feihong,Wang, Xiaojian,Liu, Zongliang,Yang, Qian,Zhang, Xiaojin,Zhu, Jia,Qiang, Lei,Guo, Qinglong,You, Qidong
, p. 110 - 123 (2012/07/28)
Previously we have reported a series of gambogic acid's analogs and have identified a compound that possessed comparable in vitro growth inhibitory effect as gambogic acid. However, their target protein as well as the key pharmacophoric motifs on the target have not been identified yet. Herein we report that gambogic acid and its analogs inhibit the activity of IκB Kinase-beta (IKKβ) through suppressing the activation of TNFα/NF-κB pathway, which in turn induces A549 and U251 cell apoptosis. IKKβ can serve as one of gambogic acid's targets. The preparation of the compounds was carefully discussed in the article. Caged 4-oxa-tricyclo[4.3.1.03,7]dec-2-one xanthone, which was identified as the pharmacophoric scaffold, represents a promising therapeutic agent for cancer and useful probe against NF-κB pathway.