18735-82-5

Usage

Uses

Used in Pharmaceutical Industry:
7-Bromo-4-hydroxy-2H-chromen-2-one is used as a pharmaceutical intermediate for the development of new drugs due to its potential biological activities, such as antioxidant and anti-inflammatory properties.
Used in Drug Development:
7-Bromo-4-hydroxy-2H-chromen-2-one is used as a drug candidate for the treatment of various diseases, given its potential therapeutic effects and ongoing research into its properties.
Used in Research and Development:
7-Bromo-4-hydroxy-2H-chromen-2-one is used as a subject of research and development in the pharmaceutical and medical fields to explore its full potential and possible applications in treating different conditions.

Upstream product

• 30186-18-6 4'-bromo-2'-hydroxyacetophenone 
• 105-58-8 Diethyl carbonate 
• 35065-86-2 3-bromophenyl acetate 
• 651780-07-3 ethyl 3-(4-bromo-2-hydroxyphenyl)-3-oxopropanoate 

Downstream Products

• 540750-32-1 2-(6-bromobenzo[d]isoxazol-3-yl)acetic acid 

Relevant academic research and scientific papers

Novel conjugates of podophyllotoxin and coumarin: Synthesis, cytotoxicities, cell cycle arrest, binding CT DNA and inhibition of Topo IIβ

A series of conjugates of podophyllotoxin and coumarin were prepared using the click reaction, and their cytotoxicities against A549, HepG2, HeLa, and LoVo cells were evaluated. Among them, compound 14e exhibited the strongest cytotoxicities against these cancer cells with IC50 values of 4.9–17.5 μM. Furthermore, 14e disrupted microtubules and induced cell cycle arrest at G1 phase by regulating P21 and Cyclin D1 in LoVo cells. In addition, 14e bond CT DNA and selectively inhibited Topo IIβ over Topo IIα. Molecular docking model showed that 14e appeared to form stable hydrogen bonds with several DNA bases and residue Gln778. Taken together, these conjugates have the potential to be developed as anti-tumor drugs.

A novel NAE/UAE dual inhibitor LP0040 blocks neddylation and ubiquitination leading to growth inhibition and apoptosis of cancer cells

NEDD8 activating enzyme (NAE) plays an important role in regulating intracellular proteins with key parts in a broad array of cellular functions. On the basis of previously work, a series of 2H-chromen-2-one based NAE inhibitors were designed and synthesized. Through enzyme-based and cell-based assays, LP0040 was identified as a non-nucleoside NAE/UAE dual inhibitor. It could inhibit NAE/UAE activities and downregulated degradations of related substrates in AGS cells, promoting apoptosis in low micromole concentrations. LP0040 possessed anti-proliferation activities with IC50 values of 0.76–3.29 μM against multiple human cancer lines and had synergistic effect with bortezomib. Thus LP0040 represented valuable starting points for future development of NAE/UAE dual inhibitors.

Coumarin NEDD8 activating enzyme inhibitor as well as preparation method and application thereof

The invention discloses a coumarin NEDD8 activating enzyme inhibitor in the general formula I as well as pharmaceutically acceptable salts, solvate, polymorphic substances, tautomers, metabolites and prodrugs of the coumarin NEDD8 activating enzyme inhibitor. The invention further discloses an application of the coumarin NEDD8 activating enzyme inhibitor to preparation of anti-tumor drugs and a preparation method of the coumarin NEDD8 activating enzyme inhibitor. Pharmacological results show that the compound has a good effect of resisting tumor cell proliferation and is clinically applicable to preparation of drugs for treating tumors.

BENZOISOXAZOLE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION

Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors

Replacement of the core heterocycle of a defined series of chromen-4-one DNA-PK inhibitors by the isomeric chromen-2-one (coumarin) and isochromen-1-one (isocoumarin) scaffolds was investigated. Structure-activity relationships for DNA-PK inhibition were broadly consistent, albeit with a reduction of potency compared with the parent chromenone.

Novel pharmaceutical compounds

The instant invention provides compounds of Formula I which are leukotriene biosynthesis inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

THIADIAZOLE SUBSTITUTED COUMARIN DERIVATIVES AND THEIR USE AS LEUKOTRIENE BIOSYNTHESIS INHIBITOR

The instant invention provides compounds of Formula (Ia) which are leukotriene biosynthesis inhibitors, wherein X is O or S, Y is O, S, -NR6-CHR7- or -NR8-C(O)- and A is selected from 5-membered aromatic heterocyclic ring, 6-membered aromatic heterocyclic ring, naphthelenic or heterobicyclic aromatic ring system, phenyl and benzyl. A is optionally mono- or disubstituted. Compounds of Formula (Ia) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

FUSED HETEROARYL DERIVATIVES FOR USE AS P38 KINASE INHIBITORS IN THE TREATMENT OF I.A. RHEUMATOID ARTHRISTIS

Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.

Coumarin derivatives for the treatment of allergies

Pharmaceutical compositions for the treatment of allergies are produced using coumarin derivatives as the active agent. Certain of these compounds and their salts are novel.