95086-96-7

Upstream product

• 122-04-3 4-nitro-benzoyl chloride 
• 109-85-3 2-methoxyethylamine 
• 67-56-1 methanol 
• 19614-29-0 1-(p-nitrobenzoyl)aziridine 
• 62-23-7 4-nitro-benzoic acid 

Downstream Products

• 95086-97-8 N-(2-methoxyethyl)-p-aminobenzamide 
• 1316066-55-3 4-[(6-chloro-4-pyrimidinyl)amino]-N-[2-(methyloxy)ethyl]benzamide 
• 1395885-91-2 N₄-(2-chlorophenyl)-N₂-[4-N-(2-methoxyethyl)carbamoylphenyl]pyrimidine-2,4-diamine hydrochloride 

Relevant academic research and scientific papers

Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors

The o-carboxylic acid substituted bisanilinopyrimidine 1 was identified as a potent hit (Aurora A IC50 = 6.1 ± 1.0 nM) from in-house screening. Detailed structure-activity relationship (SAR) studies indicated that polar substituents at the para position of the B-ring are critical for potent activity. X-ray crystallography studies revealed that compound 1 is a type I inhibitor that binds the Aurora kinase active site in a DFG-in conformation. Structure-activity guided replacement of the A-ring carboxylic acid with halogens and incorporation of fluorine at the pyrimidine 5-position led to highly potent inhibitors of Aurora A that bind in a DFG-out conformation. B-Ring modifications were undertaken to improve the solubility and cell permeability. Compounds such as 9m with water-solubilizing moieties at the para position of the B-ring inhibited the autophosphorylation of Aurora A in MDA-MB-468 breast cancer cells.

AURORA KINASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF

Described herein are inhibitors of Aurora kinase and their use in the treatment of cancer. Methods of screening for selective inhibitors of Aurora kinases are also disclosed.

COMPOUNDS AND METHODS

Disclosed are compounds having the formula (I): wherein R1, R2, R3, R4, R5, and R6 are as defined herein, and methods of making and using the same.

Exploration of secondary and tertiary pharmacophores in unsymmetrical N,N′-diaryl urea inhibitors of soluble epoxide hydrolase

The impact of various secondary and tertiary pharmacophores on in vitro potency of soluble epoxide hydrolase (sEH) inhibitors based on the unsymmetrical urea scaffold 1 is discussed. N,N′-Diaryl urea inhibitors of soluble epoxide hydrolase exhibit subtle variations in inhibitory potency depending on the secondary pharmacophore but tolerate considerable structural variation in the second linker/tertiary pharmacophore fragment.

PYRIDINYLQUINAZ0LINAMINE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS

The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Effect of para-Substituents on the Photochemical Rin-opening Reactivity of 1-(p-Substituted-benzoyl)aziridines in Methanol

Photolysis of 1-(p-substituted-benzoyl)aziridines (1a-e) in Ar-purged methanol led to N-(2-methoxyethyl)benzamides (3b-e) as the methanolysis products and/or N-ethylbenzamides (2a and b).Penta-1,3-diene quenched the formation of (2a and b) but not (3b-e).