942920-12-9

Usage

Uses

Used in Pharmaceutical Research and Development:
4-Bromo-1-ethyl-3-(4-nitrophenyl)-1H-pyrazole is utilized as a research compound for its anti-inflammatory, analgesic, and anti-cancer properties. It aids in the study of various diseases and the development of new therapeutic agents due to its ability to inhibit certain cellular processes and pathways.
Used in Organic Chemistry:
In the field of organic chemistry, 4-Bromo-1-ethyl-3-(4-nitrophenyl)-1H-pyrazole is employed as a building block for the synthesis of other compounds with potential pharmaceutical applications. Its unique structure and reactivity make it an important molecule for creating novel compounds that can be further explored for their therapeutic potential.
Used in Drug Synthesis:
4-Bromo-1-ethyl-3-(4-nitrophenyl)-1H-pyrazole is used as a key intermediate in the synthesis of pharmaceuticals, particularly those with anti-inflammatory, analgesic, and anti-cancer effects. Its role in the synthesis process is crucial for creating new drugs that can address unmet medical needs.
Used in Medicinal Chemistry:
In medicinal chemistry, 4-Bromo-1-ethyl-3-(4-nitrophenyl)-1H-pyrazole is applied as a structural template for designing new drugs. Its properties and reactivity allow chemists to modify its structure to optimize its therapeutic effects and minimize potential side effects, leading to the development of more effective and safer medications.

Upstream product

• 75-03-6 ethyl iodide 
• 73227-97-1 4-bromo-3-(4-nitrophenyl)-1H-pyrazole 

Downstream Products

• 942920-11-8 1-ethyl-3-(4-nitrophenyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole 
• 942920-52-7 [4-(4-bromo-1-ethyl-1H-pyrazol-3-yl)phenyl]amine 
• 942919-31-5 4-[1-ethyl-3-(4-nitrophenyl)-1H-pyrazol-4-yl]-1H-pyrrolo-[2,3-b]pyridine 

Relevant academic research and scientific papers

Discovery of GSK1070916, a potent and selective inhibitor of aurora B/C kinase

The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may provide a new therapy for the treatment of tumors with Aurora kinase amplification. Herein we describe our lead optimization efforts within a 7-azaindole-based series culminating in the identification of GSK1070916 (17k). Key to the advancement of the series was the introduction of a 2-aryl group containing a basic amine onto the azaindole leading to significantly improved cellular activity. Compound 17k is a potent and selective ATP-competitive inhibitor of Aurora B and C with Ki* values of 0.38 ± 0.29 and 1.5 ± 0.4 nM, respectively, and is >250-fold selective over Aurora A. Biochemical characterization revealed that compound 17k has an extremely slow dissociation half-life from Aurora B (>480 min), distinguishing it from clinical compounds 1 and 2. In vitro treatment of A549 human lung cancer cells with compound 17k results in a potent antiproliferative effect (EC50 = 7 nM). Intraperitoneal administration of 17k in mice bearing human tumor xenografts leads to inhibition of histone H3 phosphorylation at serine 10 in human colon cancer (Colo205) and tumor regression in human leukemia (HL-60). Compound 17k is being progressed to human clinical trials.

AZAINDOLE INHIBITORS OF AURORA KINASES

The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including s