153863-34-4

Usage

Uses

Used in Pharmaceutical Industry:
CHEMBRDG-BB 4010495 is used as a therapeutic agent for the treatment of cancer. It targets the PARP enzyme, which is instrumental in DNA repair mechanisms, thereby enhancing the effectiveness of DNA-damaging therapies such as chemotherapy or radiation. This application is based on the rationale that inhibiting PARP can lead to the accumulation of DNA damage in cancer cells, ultimately resulting in cell death.
Used in Oncology:
CHEMBRDG-BB 4010495 is used as a PARP inhibitor for the treatment of various types of cancer. Its application in oncology is due to its ability to synergize with DNA-damaging agents, making it a promising candidate for combination therapies that can improve patient outcomes, especially in cases of chemoresistant tumors.
Used in Neurodegenerative Disease Research:
CHEMBRDG-BB 4010495 is used as a potential neuroprotective agent in the treatment of neurodegenerative diseases. Its application in this field is based on the hypothesis that its PARP-inhibiting properties may offer protective effects against neuronal damage and degeneration, although more research is needed to confirm these effects and their clinical relevance.
Further studies are necessary to fully elucidate the pharmacological properties and therapeutic potential of CHEMBRDG-BB 4010495, ensuring its safe and effective use in various medical applications.

InChI:InChI=1/C10H9FN2O/c11-9-1-3-10(4-2-9)13-6-8(7-14)5-12-13/h1-6,14H,7H2

Upstream product

• 138907-73-0 ethyl 1-(4-fluorophenyl)-1H-pyrazole-4-carboxylate 
• 890652-03-6 1-(4-fluorophenyl)-1H-pyrazole-4-carbaldehyde 
• 371-14-2 4-fluorophenylhydrazine 

Downstream Products

• 153863-44-6 [1-(4-Fluoro-phenyl)-1H-pyrazol-4-yl]-acetonitrile 
• 153863-64-0 4-(bromomethyl)-1-(4-fluorophenyl)-1H-pyrazole 

Relevant academic research and scientific papers

Palladium Catalysis Enables Benzylation of α,α-Difluoroketone Enolates

A palladium-catalyzed decarboxylative benzylation reaction of α,α-difluoroketone enolates is reported, in which the key C(α)?C(sp3) bond is generated by reductive elimination from a palladium intermediate. The transformation provides convergent access to α-benzyl-α,α-difluoroketone-based products, and should be useful for accessing biological probes.

Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains

Recently described biphenyl analogues of the antituberculosis drug PA-824 displayed improved potencies against M. tuberculosis but were poorly soluble. Heterobiaryl analogues of these, in which the first phenyl ring was replaced with various 5-membered ring heterocycles, were prepared with the aim of identifying potent new candidates with improved aqueous solubility. The compounds were constructed by coupling the chiral 2-nitroimidazooxazine alcohol with various halomethyl-substituted arylheterocycles, by cycloadditions to a propargyl ether derivative of this alcohol, or by Suzuki couplings on haloheterocyclic methyl ether derivatives. The arylheterocyclic compounds were all more hydrophilic than their corresponding biphenyl analogues, and several showed solubility improvements. 1-Methylpyrazole, 1,3-linked-pyrazole, 2,4-linked-triazole, and tetrazole analogues had 3- to 7-fold higher MIC potencies against replicating M. tb than predicted by their lipophilicities. Two pyrazole analogues were >10-fold more efficacious than the parent drug in a mouse model of acute M. tb infection, and one displayed a 2-fold higher solubility. 2009 American Chemical Society.