923283-86-7

Usage

Type of compound

Nitro-substituted Pyrazole derivative

Common uses

Synthesis of pharmaceuticals and agrochemicals

Biological activities

Anti-inflammatory, analgesic, and anti-platelet aggregation properties

Reactivity

Diverse reactivity and functional groups, used as a building block in the synthesis of various organic compounds

Precautions

May pose health risks if not managed properly

Upstream product

• 75-30-9 2-iodo-propane 
• 138786-86-4 methyl 4-nitro-1H-pyrazole-3-carboxylate 
• 138786-86-4 4-nitro-2H-pyrazole-3-carboxylic acid methyl ester 
• 67-63-0 isopropyl alcohol 
• 67-56-1 methanol 
• 5334-40-7 4-nitro-1H-pyrazole-5-carboxylic acid 
• 5334-40-7 4-nitro-1H-pyrazole-3-carboxylic acid 

Relevant academic research and scientific papers

Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents

We pursued serine palmitoyltransferase (SPT) inhibitors as novel cancer therapeutic agents based on a correlation between SPT inhibition and growth suppression of cancer cells. High-throughput screening and medicinal chemistry efforts led to the identification of structurally diverse SPT inhibitors 4 and 5. Both compounds potently inhibited SPT enzyme and decreased intracellular ceramide content. In addition, they suppressed cell growth of human lung adenocarcinoma HCC4006 and acute promyelocytic leukemia PL-21, and displayed good pharmacokinetic profiles. Reduction of 3-ketodihydrosphingosine, the direct downstream product of SPT, was confirmed under in vivo settings after oral administration of compounds 4 and 5. Their anti-tumor efficacy was observed in a PL-21 xenograft mouse model. These results suggested that SPT inhibitors might have potential to be effective cancer therapeutics.

HETEROCYCLIC COMPOUND

The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).

PYRAZOLOPYRIMIDINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

PYRROLOPYRIDAZINE INHIBITORS OF IRAK4 ACTIVITY

The present invention relates to pyrrolopyridazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.

Pyrazolo pyrimidines useful as aurora kinase inhibitors

The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: wherein one of is a double bond, as valency permits; and R2, R4, X1A, X2A, X1B, X2B, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.