58730-35-1

Usage

Uses

Used in Pharmaceutical Research and Development:
2-(3-aminophenyl)-N-methylacetamide (SALTDATA: FREE) serves as a key starting material in the synthesis of various pharmacologically active compounds. Its unique structure allows for the creation of new drugs with potential therapeutic benefits.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 2-(3-aminophenyl)-N-methylacetamide (SALTDATA: FREE) is utilized for the exploration of its biological activities. Its structural features make it a candidate for further investigation into its potential as a therapeutic agent.
Used in Drug Discovery:
2-(3-aminophenyl)-N-methylacetamide (SALTDATA: FREE) is employed in drug discovery processes to identify new lead compounds with possible medicinal applications. Its presence in the synthesis of pharmacologically active substances underscores its importance in developing novel treatments.
Used in Chemical Synthesis:
In the chemical synthesis industry, 2-(3-aminophenyl)-N-methylacetamide (SALTDATA: FREE) is used as an intermediate in the production of complex organic molecules, leveraging its reactive functional groups for further chemical transformations.
Used in Biochemical Studies:
2-(3-aminophenyl)-N-methylacetamide (SALTDATA: FREE) is utilized in biochemical studies to understand its interactions with biological systems. This can provide insights into its potential role in medicine and help in the development of targeted therapies.
Each application underscores the compound's versatility and the ongoing need for research to fully realize its potential in various industries, particularly in pharmaceuticals where its therapeutic properties are of keen interest.

Upstream product

• 19281-10-8 N-methyl-2-(3-nitrophenyl)acetamide 
• 38411-41-5 (3-nitrophenyl)acetyl chloride 
• 52913-11-8 (3-amino-phenyl)-acetic acid methyl ester 
• 74-89-5 methylamine 
• 14338-36-4 3-amino phenylacetic acid 

Downstream Products

• 58729-94-5 3-(N'-methylureido)-phenylacetic acid methylamide 
• 58730-03-3 2-[3-(3,3-Dimethyl-ureido)-phenyl]-N-methyl-acetamide 

Relevant academic research and scientific papers

2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase

Renewed interest in covalent inhibitors of enzymes implicated in disease states has afforded several agents targeted at protein kinases of relevance to cancers. We now report the design, synthesis and biological evaluation of 6-ethynylpurines that act as covalent inhibitors of Nek2 by capturing a cysteine residue (Cys22) close to the catalytic domain of this protein kinase. Examination of the crystal structure of the non-covalent inhibitor 3-((6-cyclohexylmethoxy-7H-purin-2-yl)amino)benzamide in complex with Nek2 indicated that replacing the alkoxy with an ethynyl group places the terminus of the alkyne close to Cys22 and in a position compatible with the stereoelectronic requirements of a Michael addition. A series of 6-ethynylpurines was prepared and a structure activity relationship (SAR) established for inhibition of Nek2. 6-Ethynyl-N-phenyl-7H-purin-2-amine [IC50 0.15 μM (Nek2)] and 4-((6-ethynyl-7H-purin-2-yl)amino)benzenesulfonamide (IC50 0.14 μM) were selected for determination of the mode of inhibition of Nek2, which was shown to be time-dependent, not reversed by addition of ATP and negated by site directed mutagenesis of Cys22 to alanine. Replacement of the ethynyl group by ethyl or cyano abrogated activity. Variation of substituents on the N-phenyl moiety for 6-ethynylpurines gave further SAR data for Nek2 inhibition. The data showed little correlation of activity with the nature of the substituent, indicating that after sufficient initial competitive binding to Nek2 subsequent covalent modification of Cys22 occurs in all cases. A typical activity profile was that for 2-(3-((6-ethynyl-9H-purin-2-yl)amino)phenyl)acetamide [IC50 0.06 μM (Nek2); GI50 (SKBR3) 2.2 μM] which exhibited >5-10-fold selectivity for Nek2 over other kinases; it also showed > 50% growth inhibition at 10 μM concentration against selected breast and leukaemia cell lines. X-ray crystallographic analysis confirmed that binding of the compound to the Nek2 ATP-binding site resulted in covalent modification of Cys22. Further studies confirmed that 2-(3-((6-ethynyl-9H-purin-2-yl)amino)phenyl)acetamide has the attributes of a drug-like compound with good aqueous solubility, no inhibition of hERG at 25 μM and a good stability profile in human liver microsomes. It is concluded that 6-ethynylpurines are promising agents for cancer treatment by virtue of their selective inhibition of Nek2. This journal is

Aniline pyrimidines, its preparation method and medical use (by machine translation)

The invention relates to: an aniline pyrimidine compound represented as the formula (I), a medicinal salt thereof, a prodrug thereof, and a hydrate or solvate thereof and also relates to: the preparation method of the compound, a medicine composition comp

PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH

Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:Formula (I). Wherein Q and R1-R3 are as defined herein, compositions comprising an effective amount of a Pyrazole Pyrazine Amine Compound and methods for treating or preventing inflammatory conditions, immunological conditions, cancer, neurodegenerative diseases, age-related diseases, cardiovascular diseases and metabolic conditions, or conditions treatable or preventable by inhibition of an IKK, or an IKK pathway, comprising administering an effective amount of a Pyrazole Pyrazine Amine Compound to a patient in need thereof.