4-aromatic aminoquinazoline derivative and purpose thereof

Abstract

The invention discloses a 4-aromatic aminoquinazoline derivative and a purpose thereof, wherein the 4-aromatic aminoquinazoline derivative has a structure shown as the formula (I). Pharmacological experiments indicate that the compounds or the pharmaceutically acceptable salts thereof can restrain the multiplication of multiple tumor cells. In the formula, ring A is a benzene ring, an alkylbenzene ring, a benzothiophene ring or an alkyl benzothiophene ring, R1 is hydrogen or alkoxy, n is an integer selected from 1 to 6, R2 is -NR4R5. R4 or R5 is respectively selected from hydrogen, alkyl and naphthenic base, or R4 and R5 are combined to form a substituted or unsubstituted heterolipid ring group, wherein the substituted group is an alkyl or hydroxyalkyl. R3 is an ester group, a substituted or unsubstituted aniline, substituted or unsubstituted pyridine amino, substituted or unsubstituted pyrimidine amino, substituted or unsubstituted benzyl carbamido, substituted or unsubstituted picolyl carbamido, substituted or unsubstituted pyrimidine methyl carbamido or substituted or unsubstituted naphthenic carbamido, wherein the substituted group is halogen, alkyl, phenyl or pyridyl or pyrimidyl, and preferably, the substituted group is phenyl, pyridyl or pyrimidyl.

Description

Technical field The invention belongs to the field of medicinal chemistry, and specifically relates to an Aurora kinase inhibitor, that is, a 4-arylaminoquinazoline derivative and its use. Background technique Protein Kinases (Protein Kinases) include protein serine / threonine kinase (STK) and protein tyrosine kinase (Protein Tyrosine Kinase, PTK). Among them, a new family of serine / threonine kinases involved in mitosis, the Aurora family, has been gradually recognized. They are divided into three categories: Aurora-A, Aurora-B and Aurora-C, which mainly regulate the functions of centrosomes and microtubules. Ensure the correct separation of the centrosome and the complete division of the cytoplasm. The function of Aurora kinase involves various important events of mitosis, including centrioles, spindle changes, chromosome segregation and cytokinesis. In normal cells, Aurora kinase relies on various forms of regulatory means to express and activate in specific time and space, ...

AI Technical Summary

Problems solved by technology

Although Aurora B has a strong association with tumors and plays a very important role in the mitotic process, it has not been found to be transformed in vitro and is not widely tumorigenic in vivo.

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