87488-80-0

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General Description

2-(1-Methyl-1H-pyrazol-3-yl)-phenylamine is a chemical compound with the molecular formula C11H12N4. It is an aromatic amine containing a pyrazole ring and a substituted phenyl group. 2-(1-Methyl-1H-pyrazol-3-yl)-phenylamine is used in organic synthesis and pharmaceutical research, particularly in the development of potential drug candidates. It has been studied for its potential pharmacological properties, including its role as a potential inhibitor of certain enzymes and its potential as an anti-cancer agent. Its unique structure and properties make it a valuable compound for various scientific and industrial applications.

Upstream product

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Relevant academic research and scientific papers

Discovery of novel 2,4-diarylaminopyrimidine derivatives as potent and selective epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M resistance mutation

A series of novel 2,4-diarylaminopyrimidine derivatives of AZD9291 were discovered as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. The majority of these compounds exhibited moderate to excellent EGFR T790 M/L858R inhibitory activities and comparable anti-proliferative activities against double mutant over-expressed NCI-H1975 cells to that of AZD9291. The most promising compounds 8a displayed an IC50 of 4.1 nM against EGFR L858R/T790M mutants. 8a also showed excellent cytotoxic effect against NCI-H1975 cells with an IC50 of 59 nM and 100-fold selectivity over wide-type EGFR over-expressed A431 cells. Compound 8a significantly inhibited tumor growth in NCI-H1975 xenograft models at a non-toxic dose. Docking study performed for 8a with ATP binding site of EGFR-TK showed the similar binding mode to that of AZD9291. All these results suggested that compound 8a was a potential mutant-selective EGFR inhibitor.

Pyrimidine compounds

The present invention belongs to the field of pharmaceutical synthesis, and relates to pyrimidine compounds, a preparation method and applications thereof, a pharmaceutical composition containing the pyrimidine compounds as active components, and applications of the pyrimidine compounds in preparation of antitumor drugs. The present invention discloses a pyrimidine compound having a structure represented by a formula I, wherein W is NH, R1 is a nitrogen-containing five-membered heterocyclic ring, and R2 is a nitrogen-containing basic group. According to the present invention, the pyrimidine compound can inhibit a variety of tumor cells, can particularly and selectively act on EGFRL858R/T790M lung cancer cells, and can overcome the existing EGFR inhibitors, wherein the IC50 of the compounds is increased by 10-100 times compared to wild-type cells. The formula I is defined in the specification.

Imidazoline derivatives as alpha-1A adrenoceptor ligands

Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.

2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: α1a subtype selective 2′-heteroaryl compounds

The structure-activity relationship of 2′-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as α1 adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent α1A subtype selective agonists have been identified.