50439-63-9

Upstream product

• 528-21-2 2',3',4'-trihydroxyacetophenone 
• 100-44-7 benzyl chloride 
• 100-39-0 benzyl bromide 
• 87-66-1 2-hydroxyresorcinol 

Downstream Products

• 96755-21-4 (E)-3-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1-(2,3,4-tris-benzyloxy-phenyl)-propenone 
• 700843-42-1 2',3',4'-tribenzyloxy-4-(diethoxymethyl)chalcone 
• 700843-51-2 7,8-dibenzyloxyflavone-4'-carbaldehyde 
• 700843-53-4 3',4'-dibenzyloxy-2'-hydroxychalcone-4-carbaldehyde 
• 700843-50-1 2',3',4'-tribenzyloxychalcone-4-carbaldehyde 
• 500866-00-2 C₂₉H₂₂O₄ 
• 93827-33-9 C₂₉H₂₄O₄ 
• 38183-03-8 7,8-dihydroxyflavone 
• 2652-27-9 1-(3,4-bis(benzyloxy)-2-hydroxyphenyl)ethanone 
• 147711-26-0 7,8,4'-Trihydroxyflavone 
• 1610522-93-4 7,8-bis(benzyloxy)-4-hydroxy-2H-chromen-2-one 
• 96754-80-2 [(2S,3R)-3-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-oxiranyl]-(2,3,4-tris-benzyloxy-phenyl)-methanone 

Relevant academic research and scientific papers

Bisphosphonate-Linked TrkB Agonist: Cochlea-Targeted Delivery of a Neurotrophic Agent as a Strategy for the Treatment of Hearing Loss

Hearing loss affects more than two-thirds of the elderly population, and more than 17% of all adults in the U.S. Sensorineural hearing loss related to noise exposure or aging is associated with loss of inner ear sensory hair cells (HCs), cochlear spiral ganglion neurons (SGNs), and ribbon synapses between HCs and SGNs, stimulating intense interest in therapies to regenerate synaptic function. 7,8-Dihydroxyflavone (DHF) is a selective and potent agonist of tropomyosin receptor kinase B (TrkB) and protects the neuron from apoptosis. Despite evidence that TrkB agonists can promote survival of SGNs, local delivery of drugs such as DHF to the inner ear remains a challenge. We previously demonstrated in an animal model that a fluorescently labeled bisphosphonate, 6-FAM-Zol, administered to the round window membrane penetrated the membrane and diffused throughout the cochlea. Given their affinity for bone mineral, including cochlear bone, bisphosphonates offer an intriguing modality for targeted delivery of neurotrophic agents to the SGNs to promote survival, neurite outgrowth, and, potentially, regeneration of synapses between HCs and SGNs. The design and synthesis of a bisphosphonate conjugate of DHF (Ris-DHF) is presented, with a preliminary evaluation of its neurotrophic activity. Ris-DHF increases neurite outgrowth in vitro, maintains this ability after binding to hydroxyapatite, and regenerates synapses in kainic acid-damaged cochlear organ of Corti explants dissected in vitro with attached SGNs. The results suggest that bisphosphonate-TrkB agonist conjugates have promise as a novel approach to targeted delivery of drugs to treat sensorineural hearing loss.

Preparation method of 7,8-dihydroxy flavone

The invention relates to a preparation method of 7,8-dihydroxy flavone, and belongs to the technical field of synthesis of medical intermediates. The preparation method comprises the following steps:by taking pyrogallol as a raw material, introducing an acetyl group to synthesize DHF1; protecting three phenolic hydroxyl groups to synthesize DHF2; selectively reducing the ortho-hydroxyl group of the acetyl group to synthesize DHF3; carrying out an aldol condensation reaction on DHF3 and benzaldehyde to prepare DHF4; carrying out a cyclization reaction under the condition of iodine catalysis toobtain DHF5; and finally carrying out a hydrolysis reaction to generate the final product. The method is simple and convenient to operate, reasonable in reaction process, low in production cost, goodin product quality, free of environmental pollution and suitable for industrial production, wherein the content of the product is higher than 98%.

Design and synthesis of 3,3′-biscoumarin-based c-Met inhibitors

A library of biscoumarin-based c-Met inhibitors was synthesized, based on optimization of 3,3′-biscoumarin hit 3, which was identified as a non-ATP competitive inhibitor of c-Met from a diverse library of coumarin derivatives. Among these compounds, 38 and 40 not only showed potent enzyme activities with IC50 values of 107 nM and 30 nM, respectively, but also inhibited c-Met phosphorylation in BaF3/TPR-Met and EBC-1 cells. This journal is the Partner Organisations 2014.

Studies on gambogic acid (IV): Exploring structure-activity relationship with IκB kinase-beta (IKKβ)

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.

[60]Fullerene-flavonoid dyads

A range of fullerene-chalcone, fullerene-flavone, and fullerene-chromone dyads, including a bis(flavonyl)-fullerene dyad, were prepared by 1,3-dipolar cycloaddition reactions of azomethine ylides to C60 and by cyclopropanation of C60 with flavonyl malonates. Synthetic and natural flavonoid derivatives were used as starting materials.

Synthesis of novel [60]fullerene-flavonoid dyads

[60]Fullerene-chalcone and [60]fullerene-flavone dyads were obtained by 1,3-dipolar cycloaddition reactions of azomethine ylides with C60.