2-amino-quinazolines plk1 (polo-like kinase1) inhibitor and application thereof

A technology of methyl quinazoline and ethyl quinazoline, applied in 2-aminoquinazoline derivatives, as Polo-like kinase 1 inhibitor field, can solve growth inhibition, apoptosis, tumor cell bipolar spindle Obstructed body formation, etc.

Inactive Publication Date: 2013-12-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Importantly, the work of many scholars has shown that knocking down PLK1 in tumor cells with antisense technology, siRNA technology or small molecule inhibitors can cause the formation of bipolar spindles in tumor cells to be blocked, growth inhibition, and even apoptosis

Method used

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  • 2-amino-quinazolines plk1 (polo-like kinase1) inhibitor and application thereof
  • 2-amino-quinazolines plk1 (polo-like kinase1) inhibitor and application thereof
  • 2-amino-quinazolines plk1 (polo-like kinase1) inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0154] N-(2-isopropylphenyl)-2-hydroxyiminoacetamide (M1)

[0155] In a 50m1 three-necked bottle, first put Na 2 SO 4 5.14g (36.2mmol) dissolved in H 2 O (20ml), then add chloral hydrate 0.98g (5.9mmol), hydroxylamine hydrochloride 1.25g (17.9mmol) in a 50ml eggplant-shaped bottle, add HCl 1ml, H 2 03ml, add 0.73g (5.4mmol) of o-isopropylaniline dropwise, become turbid, heat slightly until clarification; when both the three-necked bottle and the eggplant-shaped bottle become clear, the solution in the eggplant-shaped bottle is poured into the three-necked bottle During the process, stir mechanically, rapidly raise the temperature to 100°C, the solution gradually becomes clear from turbidity, and keep it for about 8 minutes; quickly cool down to 20°C, and a tan viscous solid appears in the solution; dissolve the viscous solid in EA, and the mother liquor with EA extraction (30ml×3), column chromatography (PE:EA=5:1), yielded 0.41g product, yield 36%, mp.105-108°C.

Embodiment 2

[0157] N-(2-methylphenyl)-2-hydroxyiminoacetamide (M2)

[0158] The preparation method was similar to M1, and 0.60 g of the sample was obtained, with a yield of 40%, and mp.119-120°C.

Embodiment 3

[0160] N-(2-Ethylphenyl)-2-hydroxyiminoacetamide (M3)

[0161] The preparation method was similar to M1, and 0.68 g of the sample was obtained, with a yield of 38%, and mp.109-111°C.

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Abstract

The invention relates to the field of medicinal chemistry, and particularly relates to 2-amino-quinazolines compounds, preparation methods of the 2-amino-quinazolines compounds, medicinal compositions containing the compounds, and medical applications of the 2-amino-quinazolines compounds and the medicinal compositions, especially applications of the 2-amino-quinazolines compounds and the medicinal compositions serving as Polo-like kinase1 inhibitors.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to 2-aminoquinazoline derivatives, their preparation methods, pharmaceutical compositions containing these compounds and their medical applications, especially as Polo-like kinase 1 (Polo-like kinase1 , use of a PLK1) inhibitor. Background technique [0002] In recent years, tumors have surpassed cardiovascular diseases and become the world's leading cause of death. The research on anti-tumor drugs has important academic and practical significance. [0003] Studies have found that almost all tumors are related to uncontrolled cell growth, blocked differentiation, and abnormal apoptosis caused by the disorder of cell cycle regulation mechanism. The frequency of tumor cell division is faster than that of normal cells, and various proteins that regulate microtubule polymerization, centrosome duplication, spindle formation, and cytokinesis are often overexpressed and their ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D401/14C07D413/12C07D413/14C07D403/12C07D239/84A61K31/517A61K31/5377A61P35/00A61P35/02
Inventor 卢帅张亮孙善亮刘海春陈亚东陆涛
Owner CHINA PHARM UNIV
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