A kind of pyridine compound and application

A compound and pyridine technology, applied in the field of pyridine compounds, can solve problems such as limiting effect, drug resistance, and many adverse reactions

Active Publication Date: 2020-05-19
XI AN JIAOTONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] At present, although some innovative progress has been made in the research of anti-angiogenic drugs, there are still the following problems: ① Regulation of angiogenesis is a network involving multiple signaling pathways. After the action of single-target drugs, angiogenesis often appears compensatory. pathway, leading to the generation of drug resistance; ②The target selectivity of the discovered anti-angiogenic drugs is not high, and there are many adverse reactions; ③Single-target anti-angiogenic drugs can only act on one link of the angiogenesis process, and the Multi-factor regulation and its complexity directly limit the effect of single-target drugs

Method used

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  • A kind of pyridine compound and application
  • A kind of pyridine compound and application
  • A kind of pyridine compound and application

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Embodiment Construction

[0026] The present invention will be described in detail below in conjunction with the drawings.

[0027] See figure 1 , The structural formula of the pyrazole compound of the present invention is:

[0028]

[0029] Where R 1 Is Cl, F, H, CH 3 , CF 3 , NH 2 or R 2 For -OCH 3 Or H. See Table 1 for details.

[0030] Table 1 The specific structure of the compound of the present invention

[0031]

[0032] R in Table 1 1 The number in represents R 1 The position of the group on the benzene ring.

[0033] See figure 1 The specific preparation process of the present invention is as follows:

[0034] Synthesis of the compound p-bromo azide (3): under ice bath conditions, dissolve 2.00 g (8.00 mmol) of p-bromo bis-bromide (2) in 20 mL anhydrous DMF, and slowly add sodium azide (azide The amount of sodium azide is 0.78g (11.99mmol)), then it is raised to room temperature and then slowly added dropwise an aqueous solution of sodium azide (0.78g (11.99mmol) of sodium azide). After the addition...

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Abstract

The invention provides a pyridine compound and application. Based on the find of VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2), EphB4 (Ephrin type-B receptor 4) and TIE-2 compensatory activation, biphenyl arylurea is used as a novel leading compound to analyze conservative conformations of three receptor active sites and find out a general structure region; a molecular hybridization medicine design strategy is adopted to construct a compound library meeting the requirements of the conformations of the general structure region; multi-level activity screening finds out a multi-target inhibitor capable of simultaneously resisting three compensatory paths. A kinase screening test proves that almost pyridine compounds have relatively good kinase inhibition activity; a cell proliferation test proves that almost compounds have relatively strong cell proliferation inhibition activity; structure-activity relationship analysis used as a novel medical effect segment for designing the multi-target inhibitor, and the pyridine compound can be used for preparing an anti-angiogenesis medicine.

Description

Technical field [0001] The invention relates to a pyridine compound and application. Background technique [0002] Anti-angiogenesis is mainly used in the treatment of various vascular proliferative diseases including malignant tumors. Designed to reduce blood vessel density and inhibit angiogenesis. It was initially hypothesized that anti-angiogenesis inhibitors can circumvent typical drug resistance because their target cells are genetically stable endothelial cells. However, a variety of pro-angiogenic factors induced increased tumor invasiveness and subsequent drug resistance, so not all patients benefited from anti-angiogenic therapy. [0003] In order to better determine the resistance of cancer cells, more in-depth research has been done, which allows them to overcome anti-angiogenesis strategies. The acquired resistance of anti-angiogenesis inhibitors is mainly caused by the compensatory activation of pro-angiogenic factors. The compensatory activation of pro-angiogenic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/10A61K31/4439A61P35/00
CPCA61P35/00C07D401/10
Inventor 张杰卢闻潘晓艳王嗣岑张琳解笑瑜包涛贺浪冲
Owner XI AN JIAOTONG UNIV
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