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Pyridopyrimidine ketones derivative and application in preparing antitumor drugs thereof

An anti-tumor drug, the technology of pyrimidinone, applied in the field of chemical medicine, can solve the problem that there are very few reports on anti-tumor activity, and achieve a good effect of inhibiting activity

Inactive Publication Date: 2012-07-25
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In recent years, a class of pyridopyrimidine compounds has been reported to have multiple biological activities, including antifungal, antidiarrheal, bronchodilator, antiallergic, vasodilator, antihypertensive, etc., but there are very few reports on antitumor activity

Method used

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  • Pyridopyrimidine ketones derivative and application in preparing antitumor drugs thereof
  • Pyridopyrimidine ketones derivative and application in preparing antitumor drugs thereof
  • Pyridopyrimidine ketones derivative and application in preparing antitumor drugs thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045]

[0046] Accurately weigh the 4-amino-2,6-dihydridine 5g in the 250ml round-bottomed bottle, measured 4.17g of benzenedehyde, 2.47ml of CER, add 150ml of water, slowly hear to return, add 500mg tebac, return overnight to spend overnight overnight overnight overnight, return overnight to overnight to spend overnight and overnight overnight overnight to spend overnight and overnight overnight to spend overnight and overnight overnight to spend overnight and overnight overnight to spend overnight and overnight overnight to spend overnight and overnight overnight to spend overnight and overnight overnight overnight overnight.The next morning stopped the reaction, cooled to room temperature, and filtered 7.82g of gray -white solids, with an yield of 71.2%.

[0047] 1 H-NMR (400 MHz, DMSO-D 6 ) Δ 11.473 (s, 1H), 10.918 (s, 1H), 7.649 (s, 2H), 7.407 (m, 3H), 7.249 (m, 2H).

[0048] Example 2: 7-amino-2,4-dione-5- (4-chlorophenyl) -1,2,3,4-tetrahydrine [2,3-D] pyrimidine -6-腈 (3B)...

Embodiment 2

[0049]

[0050] The preparation method is the same as the embodiment 1, with a rate of 62.3%.

[0051] 1 H-NMR (400 MHz, DMSO-D 6 ) Δ 11.517 (s, 1H), 10.979 (s, 1H), 7.702 (s, 2H), 7.48 (D, J = 8.4Hz, 2H), 7.30 (D, J = 8Hz, 2H).

[0052] Example 3: 7-amino-2,4-dione-5- (3,4-di oxygen-phenyl) -1,2,3,4-tetrahydrine [2,3-D] pyrimidine-6-Preparation of 3 (3C)

Embodiment 3

[0053]

[0054] The preparation method is the same as the embodiment 1, with a rate of 66.1%.

[0055] 1 H-NMR (400 MHz, DMSO-D 6 ) Δ 11.433 (s, 1H), 10.911 (s, 1H), 7.601 (s, 2H), 6.98 (D, J = 8.4Hz, 1H), 6.89 (D, J = 1.6Hz, 1H), 6.811 (DD, J = 1.6Hz, J = 8Hz, 1H), 3.81 (s, 3H), 3.714 (s, 3H).

[0056] Example 4: 7-amino-2,4-dione-5- (3-methoxy-4-hydroxyl-phenyl) -1,2,3,4-tetrahydrine [2,3-D]Preparation of Pyrimidine-6-d (3D)

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Abstract

The invention relates to pyridopyrimidine ketones derivatives and application of the pyridopyrimidine ketones derivatives in preparing antitumor drugs, belongs to the chemical pharmaceutical area, particularly relates to application of a compound with a structure shows as formula (I), wherein Ar represents a substituted benzene ring or a heterocyclic ring Het; R1 represents H or CH3; and R2 represents a substituted benzene ring, a heterocyclic ring or alkane. Experiments show that compound with a structure shown as formula (I) has varying degrees of inhibitory activity in vitro to A549 (human lung adenocarcinoma cell), HepG2 (human hepatocellullar carcinoma cell), SKOV-3 (human ovarian neoplasm), Hela (human cervical carcinoma cell) and SW620 (human colonic cancer cell), and in particular has good inhibitory activity to SW620, so that a new choice is provided for preparation of the antitumor drugs.

Description

Technical field [0001] The present invention is a chemical medicine field, which specializes in a type of pyridine and pyrine derivatives and the use of anti -tumor drugs. Background technique [0002] Cancer, also known as Malignant Neoplasm, is caused by the disorders of the cell growth and proliferation mechanism. [0003] Entering the 21st century, malignant tumors are still an important disease that affects human life and health. Its mortality rate is rising year by year. The mortality rate of malignant tumors in my country is a high level in the world.Therefore, malignant tumors have become an important disease that seriously threaten human health and social development in my country. [0004] Malignant tumor treatment is mainly divided into surgical treatment and chemotherapy.Surgical treatment is the most important effective treatment for many early and medium -term physical tumors. About 60%of physical tumors use surgery as the main treatment method.However, for the exis...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07D519/00A61K31/519A61K31/522A61P35/00
Inventor 罗有福魏于全
Owner SICHUAN UNIV