5928-35-8

Upstream product

• 67047-05-6 4-oxo-2-phenyl-4H-1-benzopyran-5,6,7-triyl triacetate 
• 21967-41-9 baicalin 
• 491-67-8 5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one 
• 100-39-0 benzyl bromide 
• 67047-06-7 7-(benzyloxy)-4-oxo-2-phenyl-4H-1-benzopyran-5,6-diyl diacetate 

Downstream Products

• 1272971-84-2 5-hydroxy-6-(2-morpholin-4-yl-ethoxy)-7-benzyloxy-flavone 
• 1345982-19-5 5,7-dihydroxy-6-(2-morpholin-4-yl-ethoxy)-flavone 
• 1357354-99-4 7-(benzyloxy)-5-hydroxy-4-oxo-2-phenyl-4H-1-benzopyran-6-yl 2-hydroxyacetate 
• 1357354-97-2 7-(benzyloxy)-6-(2-hydroxyethoxy)-5-methoxy-2-phenyl-4H-1-benzopyran-4-one 
• 1357354-95-0 7-(benzyloxy)-5-hydroxy-6-(2-hydroxyethoxy)-2-phenyl-4H-1-benzopyran-4-one 
• 1263322-72-0 7-(benzyloxy)-6-(3-(dimethylamino)-propoxy)-5-hydroxy-2-phenyl-4H-chromen-4-one 
• 1263322-73-1 7-(benzyloxy)-5-hydroxy-2-phenyl-6-(3-(pyrrolidin-1-yl)propoxy)-4H-chromen-4-one 
• 1263322-74-2 C₃₀H₃₁NO₅ 
• 1263322-75-3 C₂₉H₂₉NO₆ 
• 1263322-76-4 C₃₀H₃₂N₂O₅ 
• 1263322-93-5 C₂₄H₂₇NO₅ 
• 1571989-59-7 C₁₉H₁₆O₅ 
• 1263322-87-7 C₂₃H₂₅NO₅ 
• 1263322-88-8 C₂₄H₂₇NO₅ 

Relevant academic research and scientific papers

Design, synthesis, and primary activity assays of baicalein derivatives as cyclin-dependent kinase 1 inhibitors

Malignant tumor is a disease with high mortality. Traditional treatment methods have many disadvantages, such as side-effects, drug resistance. Because cyclin-dependent kinase 1 (CDK1) plays an indispensable role in cell cycle regulation, it became an att

Synthetic method of oroxylin

The invention relates to a synthetic method of oroxylin. The method disclosed by the invention comprises the following steps: carrying out acetylation reaction on 5, 6, 7-trihydroxy flavone and aceticanhydride in pyridine at room temperature; reacting an obtained acetylate with benzyl bromide or benzyl chloride in the presence of an inorganic base, and carrying out hydrolysis reaction on a product in alkaline water; and reacting with methyl iodide in the presence of an inorganic base, and finally debenzylating in the presence of concentrated sulfuric acid to obtain the target product oroxylin. The method for synthesizing oroxylin provided by the invention has the advantages of simple and feasible operation, high product purity, high reaction yield and the like, and is easier for industrial production compared with the existing method.

Anti-angiogenic and anticancer effects of baicalein derivatives based on transgenic zebrafish model

Angiogenesis leads to tumor neovascularization by promoting tumor growth and metastatic spread, therefore, angiogenesis is considered as an attractive target for potential small molecule anticancer drug discovery. Herein, we report the structural modification and biological evaluation of baicalein derivatives, among which compound 42 had potent in vivo anti-angiogenic activity and wide security treatment window in transgenic zebrafish model. Further, 42 exhibited the most potent inhibitory activity on HUVEC proliferation, migration and tube formation in vitro. Moreover, 42 significantly inhibited growth of human lung cancer A549 cells and weak influence on human normal fibroblast L929 cells. The present research demonstrated that the significant anti-angiogenic and anticancer effects, which provided the supportive evidence for 42 could be used as a potential compound of cancer therapy.

Synthesis and biological evaluation of baicalein derivatives as potent antitumor agents

Baicalein (5,6,7-trihydroxy-2-phenyl-4H-chromen-4-one), a major flavonoid extracted from the root of Scutellaria baicalensis Georgi (Chinese name: Huangqin), showed potent anti-proliferative activity against a broad panel of human cancer cell lines both in vitro and in vivo. A novel series of baicalein derivatives were synthesized by introducing a group to C6-OH and a nitrogen-containing hydrophilic heterocyclic ring to C7-OH via a length of 3 or 4-carbon chain in this study. The in vitro antiproliferative activities of the 30 derivatives against HepG2, A549, BCG-823 cancer cell lines were evaluated. Among them, 10 compounds exhibit more potent cytotoxicity than baicalein against the three cancer cell lines. The most potent compound 9b possesses highest anti-proliferative potency against HepG2, A549, and BCG-823 with an IC 50 value of 2.0 μM, 0.8 μM and 3.2 μM, respectively. Preliminary mechanism studies with compound 9b using Annexin V/PI double-staining assay and DAPI staining assay indicated that 9b inhibits tumor cell proliferation potentially through inducing apoptosis.

Novel synthetic baicalein derivatives caused apoptosis and activated AMP-activated protein kinase in human tumor cells

Studies on the anti-proliferative activities of novel baicalein derivatives demonstrated that compounds 8 and 9 were able to activate AMPK by enhancing the levels of phosphorylated AMPKα, and showed more potent anti-proliferative effects than baicalein an

Synthesis of ring A-modified baicalein derivatives

Baicalein, an important active constituent of the traditional Chinese herb Scutellaria baicalensis, exhibited antitumor activity and inhibitory activity against P-gp 170. The syntheses of 25 baicalein derivatives, 2-26 (Table), are described here (Scheme