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Application of pimavanserin in preparation of antitumor drugs

An anti-tumor drug, the technology of pimaserin, applied in the field of medicine, can solve the problems of insufficient understanding, neonatal malformation, and the safety has not been well verified, and achieves the effect of good safety and low toxicity

Active Publication Date: 2021-08-20
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Thalidomide (thalidomide): Thalidomide was first launched in Germany in the 1950s for the treatment of pregnancy reactions. Due to the lack of understanding of the hand-shaped structure of the drug at that time and the lack of good safety verification in clinical trials , leading to a large number of neonatal malformations

Method used

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  • Application of pimavanserin in preparation of antitumor drugs
  • Application of pimavanserin in preparation of antitumor drugs
  • Application of pimavanserin in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021]Example 1: Preparation of pirazine forest

[0022] Step i: Take 4-hydroxybenzaldehyde to remove hydroxybenzaldehyde (12.2 g, 100 mmol), bromine isobutane (13.7 g, 100 mmol), K 2 CO 3 (69 g, 500 mmol) was placed in a 250 mL flask, and 100 ml of DMF was added, and the reaction was stirred at 80 degrees for 24 h. The reaction was stopped, poured into 800 ml of water, stir until K 2 CO 3 Dissolve, EA was extracted 3 times, combined with an organic phase and washed with 2 mol / l NaOH solution, water, saturated brine, dried over anhydrous sodium sulfate, and evaporated, to give a pale yellow liquid to isobutyl isryaldehyde 12.23 g, The yield was 68.7%.

[0023] Step II: Sodium hydrogencarbonate (4.62 g, 55 mmol), hydroxylamine (3.82 g, 55 mmol) was placed in a flask, and 30 ml of water was added, and the reaction was stirred at room temperature for 20 min to give a hydroxylamine aqueous solution. It is proud to be placed in a flask (8.91 g, 50 mmol) to the flask, and 50 ml of EtO...

Embodiment 2

[0027] Example 2: Pirazinelin inhibits the inhibitory activity of A549, MCF7, HCT116, PC3 cells

[0028] (1) Experimental materials

[0029] Cell lines: A549, MCF7, HCT116, PC3 cells were lahed in 96-well plates at 1500, 2200, 800, and 2000 / well, 100 ul, 24 h, respectively, 24 h.

[0030] 马 色 林: Diluted with DMSO, diluted with a culture medium to be prepared to be stored at -20 ° C for five different concentrations of 5 μm, 2.5 μm, and the final concentration of DMSO is below 0.1%.

[0031] Positive control: SorafeniB, 5-fluorouracil (5-Fluorouracil).

[0032] MTT: The PBS was dissolved to 2 mg / ml, stored at -20 ° C.

[0033] (2) Experimental method

[0034] With the MTT method, the A549, MCF7, HCT116, PC3 cells were selected to evaluate the anti-tumor value of the test sample. A549, HCT116, and PC3 cell line were cultured on RPMI 1640 medium, which contains 10% calf serum (FBS), and MCF-7 cell lines were cultured on DMEM medium, which contains 10% calf. Serum (FBS). When the ...

Embodiment 3

[0039] Example 3: Tablet formula

[0040] Active compound 25-1000 mg, starch 45 mg, microcrystalline cellulose 35 mg, polyvinylpyrrolidone (10% aqueous solution) 4 ml, sodium carboxymethylcellulose 4.5 mg, stearate 0.5 mg, talc 1 mg.

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Abstract

The invention relates to application of pimavanserin in preparation of antitumor drugs, belongs to the technical field of medicines, and particularly relates to novel application of pimavanserin in preparation of antitumor drugs. The structural formula of the pimavanserin is shown in the formula I. The biological activity test of the compound shows that the compound has antitumor activity and is a novel antitumor drug.

Description

Technical field [0001] The invention belongs to the field of medical technology, and specific to pimavanserin is prepared in the preparation of anti-tumor drugs. Background technique [0002] Cancer has now become a major challenge in human health and health, is an important factor that leads to human death. The occurrence of tumors is an uncontrolled cell proliferation, which is an abnormal behavior of self-cells, often related to some of the abnormal signal transduction regulatory mechanisms (Yang L, Shi P, Zhao G, et al. Signal Transductionand Targeted TargeApy 2020, 5 (1): 8-43). In the treatment of cancer, there is already a development of surgery, drug treatment, etc. However, traditional chemotherapy drugs often have strong poisonous side effects, and the adverse reactions are severe, the application range is limited, and the occurrence of small molecules is alleviated to a severe toxic side effects of chemotherapy drugs to some extent, but with the prolongation time, Targ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4468A61P35/00C07D211/58
CPCA61K31/4468A61P35/00C07D211/58
Inventor 胡春侯世澄刘聪翀张冰琦李泰张传明邓新山金辄李涛刘晓平黄二芳李凤荣
Owner SHENYANG PHARMA UNIVERSITY
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