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HIF-1[alpha] inhibition antitumor candidate drug and preparation method thereof

A candidate drug, HIF-1 technology, applied in the field of malignant tumors, can solve the problem of poor effect of vascular blockers

Inactive Publication Date: 2017-07-14
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The purpose of the present invention is to provide a preparation method of an anti-tumor candidate drug that inhibits HIF-1α, aiming to solve the problem that in clinical medicine, the effect of using blood vessel blocking agents alone is not good, and the tumor blood vessels can still survive after blocking

Method used

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  • HIF-1[alpha] inhibition antitumor candidate drug and preparation method thereof
  • HIF-1[alpha] inhibition antitumor candidate drug and preparation method thereof
  • HIF-1[alpha] inhibition antitumor candidate drug and preparation method thereof

Examples

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preparation example Construction

[0020] Such as figure 1 As shown, the preparation method of the anti-tumor candidate drug for inhibiting HIF-1α provided by the embodiment of the present invention includes the following steps:

[0021] S101: Add Chrysin (2.54g, 0.01mol), anhydrous potassium carbonate (5.52g, 0.04mol) and acetone (100ml) in a 250mL round-bottom flask, heat and stir to reflux, then add 1,2-two dropwise Bromoethane or 1,3-dibromopropane or 1,4-dibromobutane (0.04mol), heated to reflux at 60°C, the solution became clear and then turbid. TCL (Thin Layer Chromatography) was used to detect the progress of the reaction, and purified by column chromatography. The eluent was methanol: dichloromethane=1:50.

[0022] S102: Add the benzimidazole derivative (0.015mol) into a 250mL three-necked flask, dissolve it in 100mL of acetone, add potassium carbonate (5.52g, 0.04mol), stir for 10min, add the purified chrysin derivative obtained in step 1 (0.01mol), tetrabutylammonium bromide (TBAB) (0.03g, 0.0001mol), he...

Embodiment 1

[0026] Example 1: 7-(2-Bromoethoxy)-5-hydroxy-2-phenyl-4H-benzopyrone-4-one

[0027] In a 250mL round-bottom flask, add chrysin (2.54g, 0.01mol), anhydrous potassium carbonate (5.52g, 0.004mol) and acetone (100ml) successively, heat and stir to reflux, and then add 1,2-dibromoethane dropwise Alkane (0.04mol), heated at 60°C to condense and reflux, the solution becomes clear and then turbid. The reaction progress was detected by TCL (Thin Layer Chromatography) and purified by column chromatography. The eluent was: methanol:dichloromethane=1:50.

[0028]

Embodiment 2

[0029] Example 2: 7-(3-Bromopropoxy)-5-hydroxy-2-phenyl-4H-benzopyrone-4-one

[0030] In a 250mL round-bottom flask, add chrysin (2.54g, 0.01mol), anhydrous potassium carbonate (5.52g, 0.004mol) and acetone (100ml) successively, heat and stir to reflux, and then add 1,3-dibromopropane dropwise (0.04mol), heated to reflux at 60°C, the solution becomes clear and then turbid. The reaction progress was detected by TCL (Thin Layer Chromatography) and purified by column chromatography. The eluent was: methanol:dichloromethane=1:50.

[0031]

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Abstract

The invention discloses a HIF-1[alpha] inhibition antitumor candidate drug and a preparation method thereof. According to the present invention, a compound to be designed and synthesized can inhibit the glycolysis ability of tumor cells, the glycolysis inhibition adopts hypoxia-inducible factor 1[alpha] as the target, a flavone natural compound is designed and synthesized as a mother nucleus, the mother nucleus is modified with a benzimidazole derivative to synthesize series chrysin derivatives, and screening is performed by using the inhibition level of in vitro antitumor activity target protein to obtain the compound acting on the hypoxia-inducible factor 1[alpha]; the candidate drug inhibiting the glycolysis is selected; and the new potential candidate drug is provided for tumor treatment.

Description

Technical field [0001] The invention belongs to the technical field of malignant tumors, and particularly relates to an anti-tumor candidate drug for inhibiting HIF-1α and a preparation method. Background technique [0002] Tumor is a common and frequently occurring disease, among which malignant tumors currently have the most serious harm to human health. Blood vessels provide enough oxygen and nutrients for tumor growth and survival, and eliminate metabolic waste. Therefore, tumor vascular targeted therapy has become an effective tumor treatment strategy. Research progress of tumor vascular inhibitors In the early 1970s, Folkman first proposed that tumor neovascularization plays an important role in tumor growth and spread. Further research by Bergers et al. also showed that tumor cells need the support of new blood vessels and functional blood vessels during proliferation and metastasis; moreover, a large number of studies in recent years have confirmed that tumor growth and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12A61P35/00
CPCC07D405/12
Inventor 邓湘萍唐国涛王哲曹轩熊淑娟熊润德刘娟邹柳
Owner NANHUA UNIV
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