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Application of pyrazolopyrimidine compound in preparation of transcription inhibitor medicine

A technology of pyrazolo and inhibitors, applied in the field of pyrazolopyrimidine compounds in the preparation of transcription inhibitor drugs, which can solve the toxic and side effects of human body, the curative effect and prognosis of tumor treatment are not very ideal, and do not have tumor specificity and other problems, to achieve the effect of definite curative effect and good clinical application prospect

Inactive Publication Date: 2014-03-26
LUZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although cervical cancer is the only cancer for which the cause of the disease has been found so far, its treatment is still consistent with the general tumor treatment plan. Both chemotherapy and radiotherapy are used. Conventional radiotherapy and chemotherapy are basically not specific for tumors. Cells also have a killing effect on normal cells at the same time, thereby causing great toxic and side effects to the human body, and at the same time leading to the destruction of the host immune system. After radiotherapy and chemotherapy, it is easy to cause various complications and the tumor is easy to relapse. The characteristics of conventional radiotherapy and chemotherapy The curative effect and prognosis of tumor treatment are not very ideal

Method used

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  • Application of pyrazolopyrimidine compound in preparation of transcription inhibitor medicine
  • Application of pyrazolopyrimidine compound in preparation of transcription inhibitor medicine
  • Application of pyrazolopyrimidine compound in preparation of transcription inhibitor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Experiment of Compound C inhibiting transcription

[0031] 1. Experimental method

[0032] (1) Commercially available tumor cells A549, SMMC-7721 and HeLa were taken and cultured;

[0033] The specific culture method is as follows: culture cells in DMEM medium with 10% fetal bovine serum, place in CO 2 in an incubator (5% CO 2 , 95% air, 37°C), change the liquid according to the situation;

[0034] (2) The above cells were treated with 0, 5, and 10 μM / L doses of Compound C, and 3H-uridine (3H-uridine) was added to the medium for 24 hours, and the transcription inhibitor DRB (5 ,6-dichloro-1-β-D-ribofuranosylbenzimidazole) as a positive control;

[0035] (3) Use a liquid scintillation instrument to analyze the amount of 3H-uridine in the cells, and analyze the transcription level.

[0036] 2. Experimental results

[0037] Cells need to use uridine for transcription. Therefore, when 3H-uridine is added to the medium, the higher the cell transcription level...

Embodiment 2

[0040] Example 2 The Experiment of Compound C Promoting Tumor Cell Apoptosis

[0041] 1. Experimental method

[0042] 1.1 Effects of different concentrations of Compound C on apoptotic proteins (PARP, cleaved Caspase-3)

[0043] (1) Commercially available tumor cells A549, SMMC-7721 and HeLa were taken and cultured;

[0044] The specific culture method is as follows: culture cells in DMEM medium with 10% fetal bovine serum, place in CO 2 in an incubator (5% CO 2 , 95% air, 37°C), change the liquid according to the situation;

[0045] (2) Treat the above cells with 0, 2.5, 5, and 10 μm / L doses of Compound C respectively for 24 hours, and collect the cells;

[0046] (3) Cells were taken, lysed, and the obtained lysate was quantified by BCA method, and then denatured by SDS;

[0047] (4) Analyze the above protein samples by SDS-PAGE and Western blot to determine the effect of Compound C on the two apoptotic proteins.

[0048] 1.2 Effects of Compound C treatment for differen...

Embodiment 3

[0069] Example 3 Experiment of Compound C Inhibiting Tumor Formation of Tumor Cells in Vivo

[0070] 1. Experimental animals

[0071] Source and strain: BALB / c-nu nude mice were purchased from the Experimental Animal Center of Second Military Medical University.

[0072] Age, weight: 6 weeks old, about 20g.

[0073] Gender: Male.

[0074] Number of animals: 6 per group.

[0075] 2. Experimental method

[0076] (1) Take commercially available tumor cells A549 and SMMC-7721 and culture them;

[0077] The specific culture method is as follows: culture cells in DMEM medium with 10% fetal bovine serum, place in CO 2 in an incubator (5% CO 2 , 95% air, 37°C) culture;

[0078] (2) Feeding 6-week-old nude mice;

[0079] (3) Take A549 and SMMC-7721 cells and inoculate them subcutaneously in nude mice (cell injection volume is 1×10 7 / Only);

[0080] (4) After 7 days of subcutaneous injection, the experimental group was injected with Compound C intratumorally at a dose of 15 ...

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Abstract

The invention discloses an application of 6-[4-[2-(1-piperidyl)ethoxy]phenyl]-3-(4-pyridyl)pyrazolo[1,5-A]pyrimidine in preparation of a transcription inhibitor medicine. The invention also discloses a pharmaceutical composition which is a preparation prepared by taking 6-[4-[2-(1-piperidyl)ethoxy]phenyl]-3-(4-pyridyl)pyrazolo[1,5-A]pyrimidine as an active ingredient accompanied by pharmaceutically acceptable accessories or auxiliary components. The 6-[4-[2-(1-piperidyl)ethoxy]phenyl]-3-(4-pyridyl)pyrazolo[1,5-A]pyrimidine disclosed by the invention can effectively inhibit cell transcription and induce tumor cell apoptosis, realizes an exact curative effect on lung cancer, liver cancer or cervical cancer, and has a good prospect in clinical application.

Description

technical field [0001] The present invention relates to 6-[4-[2-(1-piperidyl)ethoxy]phenyl]-3-(4-pyridyl)pyrazolo[1,5-A]pyrimidine in the preparation of transcription inhibitors use in . Background technique [0002] Compound C, also known as dorsomorphin, 6-[4-[2-(1-piperidinyl)ethoxy]phenyl]-3-(4-pyridyl)pyrazolo[1,5-A]pyrimidine , is a natural small molecular substance isolated from substances related to the formation of the dorsal-ventral axis of zebrafish. Compound C is a potent inhibitor of 5'-adenosine phosphate-activated protein kinase (AMP-activated protein kinase, AMPK) and bone morphogenic protein (Bone morphogenetic protein, BMP) signaling pathways (Zhou G, Myers R, Li Y, et al .Role of AMP-activated protein kinase in mechanism of metformin action.J.Clin.Invest.2001;108(8):1167-1174;Yu PB,Hong CC,Sachidanandan C,et al.Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.Nat.Chem.Biol.2008;4(1):33-41.), can regulate the energy metabo...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P35/00A61P11/00A61P1/16A61P15/00
Inventor 代荣阳冯春红贺凯陈润刘友平段春燕张春燕
Owner LUZHOU MEDICAL COLLEGE
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