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Application of indazole hydrazide compound in preparation of anti-tumor angiogenesis medicine

An indazole hydrazide, angiogenesis technology, applied in antitumor drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as drug resistance, and achieve the effect of inhibiting angiogenesis

Inactive Publication Date: 2021-07-13
PEKING UNIV FIRST HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The VEGF family and its receptors play an important role in the process of tumor angiogenesis. Therefore, inhibiting the activity of the VEGF family and its receptors, thereby inhibiting the transmission of downstream signaling molecules, can effectively inhibit tumor angiogenesis, but it must be combined with chemotherapy drugs. Combined use, and long-term use will lead to drug resistance

Method used

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  • Application of indazole hydrazide compound in preparation of anti-tumor angiogenesis medicine
  • Application of indazole hydrazide compound in preparation of anti-tumor angiogenesis medicine
  • Application of indazole hydrazide compound in preparation of anti-tumor angiogenesis medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Prepare the compound shown in formula (1) ~ formula (5) according to the following steps:

[0065]

[0066] Ph represents a substituted or unsubstituted phenyl group.

[0067] Sodium ethoxide solution was prepared by adding sodium (1.5 g, 65 mmol) to absolute ethanol (20 mL) at 0 °C; then a mixture of cyclohexanone (4.41 g, 44 mmol) and diethyl oxalate (7.3 g, 50 mmol) was added slowly , and stirred the solution at room temperature for 12 h, and then decomposed the reaction mixture with 2N sulfuric acid solution, extracted the mixture with ethyl acetate, dried and concentrated the organic solvent, and the obtained crude product was columnar with n-hexane:ethyl acetate (12:1) Further purification by chromatography gave yellow oil as product 2 (5.87 g, 67%).

[0068] Hydrazine (448 mg, 14 mmol) was slowly added to a cooled suspension of product 2 (2.38 g, 12 mmol) in acetic acid (5 mL), the mixture was heated to reflux for 1 h, poured into ice water, and washed with N...

Embodiment 2

[0093] Example 2 Determination of anti-tumor angiogenesis activity

[0094] 2.1 Evaluation of 2D angiogenesis experiments Anti-angiogenesis experiments of compounds:

[0095](1) In a 96-well plate, add 50ul of 100% Matrigel to each well to avoid air bubbles. Place in a 37°C incubator for 45 minutes.

[0096] (2) Digest well-growing HUVEC cells when their confluence reaches about 80%, and resuspend the cells with HUVEC complete medium. Add 40uL of resuspension solution to each well, the concentration is 4X10000 / well cells, repeat three wells.

[0097] (3) Add 5 uL of compounds with three concentrations of high, medium and low to the compound group to be tested. In the VEGF group, 5uL of culture solution containing 200ng / ml VEGF was added. The solvent group was supplemented with 10uL culture solution.

[0098] (4) Cultivate in a 5% CO2 incubator at 37°C for 4 hours, and take pictures of each well.

[0099] The result is as Figure 11 , Figure 12 shown.

[0100] The num...

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Abstract

The invention provides an application of an indazole hydrazide compound in preparation of an anti-tumor angiogenesis medicine. The indazole hydrazide compound has a structure as shown in a formula I which is described in the specification. According to the present invention, the anti-angiogenesis effect of the compound is evaluated on human umbilical vein vascular endothelial cells and tumor-induced angiogenesis models through the compound, and the experimental results show that the compound has significant anti-tumor angiogenesis activity. Therefore, the indazole hydrazide compound can be applied to preparation of anti-tumor angiogenesis drugs and used for inhibiting tumor angiogenesis.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to the application of an indazole hydrazide compound in the preparation of anti-tumor angiogenesis drugs. Background technique [0002] Tumor angiogenesis is closely related to tumor growth and metastasis, and anti-angiogenesis drugs have always been a hot spot in the research and development of tumor therapeutic drugs. The VEGF family and its receptors play an important role in the process of tumor angiogenesis. Therefore, inhibiting the activity of the VEGF family and its receptors, thereby inhibiting the transmission of downstream signaling molecules, can effectively inhibit tumor angiogenesis, but it must be combined with chemotherapy drugs. Combined use, and long-term use will produce drug resistance. Contents of the invention [0003] In view of this, the technical problem to be solved by the present invention is to provide an application of an indazole hydrazid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/416A61P35/00
CPCA61K31/416A61P35/00
Inventor 崔一民庞晓丛向倩周颖何旭虞巍赵侠张卓施学东解染
Owner PEKING UNIV FIRST HOSPITAL
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