90946-26-2

Upstream product

• 539-44-6 N-4-methylphenylhydrazine 
• 181294-57-5 β-formyl-β-nitroenamine 
• 34461-00-2 nitromalondialdehyde sodium salt 
• 2075-46-9 4-nitro-1H-pyrazole 
• 624-31-7 4-tolyl iodide 
• 5720-05-8 4-methylphenylboronic acid 

Downstream Products

• 1584233-85-1 7,8-dimethoxy-1-p-tolyl-1H-pyrazolo[4,3-c]isoquinoline 
• 1584233-52-2 5-(3-(trifluoromethyl)phenyl)-4-nitro-1-p-tolyl-1H-pyrazole 
• 1584233-53-3 5-(4-methoxyphenyl)-4-nitro-1-p-tolyl-1H-pyrazole 
• 1584233-54-4 4-(4-nitro-1-p-tolyl-1H-pyrazol-5-yl)benzonitrile 
• 1584233-55-5 4-nitro-1,5-di-p-tolyl-1H-pyrazole 
• 1584233-56-6 4-nitro-5-phenyl-1-p-tolyl-1H-pyrazole 
• 1584233-57-7 5-(2-fluorophenyl)-4-nitro-1-p-tolyl-1H-pyrazole 
• 1584233-66-8 2-(4-nitro-1-p-tolyl-1H-pyrazol-5-yl)pyrimidine 
• 1584233-67-9 3-(4-nitro-1-p-tolyl-1H-pyrazol-5-yl)pyridine 
• 1584233-68-0 5-(4-nitro-1-p-tolyl-1H-pyrazol-5-yl)pyrimidine 
• 1584233-74-8 4,5-dimethoxy-2-(4-nitro-1-p-tolyl-1H-pyrazol-5-yl)benzaldehyde 
• 1443247-18-4 1-[(1S,4S)-4-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydro-naphthalen-1-yl]-3-(1-p-tolyl-1H-pyrazol-4-yl)-urea 
• 1443247-90-2 (1-p-tolyl-1H-pyrazol-4-yl)-carbamic acid 2,2,2-trichloro-ethyl ester 
• 90839-86-4 4-amino-1-p-tolyl-1H-pyrazole 

Relevant academic research and scientific papers

Design and synthesis of anti-tumor compounds containing ferulic acid-pyrazole skeleton

The invention discloses design and a preparation method of an anti-tumor compound containing a ferulic acid-pyrazole skeleton. The structure of the anti-tumor compound is shown as a formula in the specification.

Design of potent B-RafV600E inhibitors by multiple copy simulation search strategy

B-Raf kinase is a vital intermedium in the mitogen-activated protein kinase (MAPK) signaling pathway, which transforms extracellular signals into cellular mechanisms. Mutations in this kinase, for instance, the most common V600E mutation, can lead to the ERK signaling pathologically activated and hence cause severe diseases such as somatic tumors. So far, the development of B-Raf inhibitors has made remarkable progress. However, the resistance and relapse of approved Raf drugs have been widely reported, and the optimization for old drugs and the discovery for new inhibitors still remain a significant task. In this study, we designed and evaluated a series of novel B-RafV600E inhibitors. A fragment library has been established before the docking simulation carried out using the MCSS strategy (multicopy simulation search). The appropriate fragments were reassembled to provide new candidate compounds, which were further screened by iterative docking simulations and molecular dynamics. Bioassays were carried out to evaluate the pharmacological profile of the compounds identified and synthesized. The result showed that compound 5n had an impressive enzyme inhibitory and antiproliferation activity, suggesting a promising potential in the future study.

Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAFV600E inhibitors

With the increasingly acquired resistance, relapse and side effects of known marketed BRAFV600E inhibitors, it's significant to design the more effective and novel drugs. In this study, a series of novel pyrazole derivatives containing acetamid

Identification and Biological Evaluation of Novel Type II B-RafV600E Inhibitors

The mitogen-activated protein kinase (MAPK) pathway plays a vital role in signal transduction networks. Severe diseases may be triggered if it is disturbed by mutated components, especially the kinase B-RafV600E. New inhibitors of the kinase ar

Regioselective and guided C-H activation of 4-nitropyrazoles

A divergent and regioselective approach to 5-aryl-4-nitro-1H-pyrazoles was developed by guided transition-metal-catalyzed arylation of 4-nitro-1H- pyrazoles. This method provides a convenient tool for the functionalization of the pharmacologically relevan

KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

KINASE INHIBITORS

Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

New synthetic equivalent of nitromalonaldehyde treatable in organic media

β-Nitroenamines having a formyl group at the β-position behave as the synthetic equivalent of unstable nitromalonaldehyde, which is a useful synthon for syntheses of versatile nitro compounds. High solubility of the nitroenamines into general organic solv