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A camphorane compound that inhibits tubulin and its preparation method and application

A tubulin and compound technology, applied in the field of chemistry, can solve problems such as difficult synthesis and complex structure, and achieve the effects of simple preparation method, easy operation, and strong anti-microtubule polymerization effect.

Active Publication Date: 2018-07-13
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the complex structure of the above-mentioned drugs and the difficulty of synthesis, the search for new and efficient microtubule inhibitors has become a hot spot in the research of anti-tumor drugs.

Method used

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  • A camphorane compound that inhibits tubulin and its preparation method and application
  • A camphorane compound that inhibits tubulin and its preparation method and application
  • A camphorane compound that inhibits tubulin and its preparation method and application

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Embodiment 1

[0031] In the embodiment of the present invention, a camphorane compound that inhibits tubulin, the structural formula of the camphorane compound is as shown in (1):

[0032]

[0033] (1), R in (1) 1 , R 3 Is an alkane group, an alkenyl group, an alkyne group, R 2 , R 4 is H, hydroxyl, alkoxy, amino or halo.

[0034] The preparation method of described camphorane compound, comprises the following steps:

[0035] 1) Preparation of crude extract from chloroform fraction

[0036] The underground part of Chrysanthemum multispike is air-dried in a cool place, then crushed to obtain coarse powder of the medicinal material, using ethanol with a volume fraction of 95% as the extraction solvent, extracting by heating and pressurizing the extraction tank at 70°C until the color of the extract is light, and then extracting together Liquid, use a rotary evaporator to recover the extraction solvent under reduced pressure, and dry it in a 60°C oven to obtain an extract. Dissolve and...

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Abstract

The invention discloses a linderane compound capable of inhibiting microtubulin and a preparation method and application of the linderane compound capable of inhibiting the microtubulin. The linderane compound is shown as the formula (I), wherein each of R1 and R3 refers to alkane group, alkylene or alkyne group, and each of R2 and R4 refers to H, hydroxyl, alkoxy, amino or halogeno. The linderane compound is capable of competing with radiolabeled colchicine in a binding site to inhibit binding of the colchicine and the microtubulin and acts in a dose-dependent manner. Both the linderane compound and the colchicine can inhibit microtubulin polymerization, and the linderane compound is powerful in antimicrotubular polymerization. The linderane compound is simple in preparation method and easy to operate and can be used for preparing various tumor treatment medicines.

Description

technical field [0001] The invention relates to the field of chemical technology, in particular to a camphorane compound that inhibits tubulin and its preparation method and application. Background technique [0002] Tubulin is the basic structural unit of intracellular microtubules. It has two types, α and β, and has various cellular functions such as maintaining cell shape, dividing cells, signal transduction and material transport. Its main function is to form the spindle during cell division. Therefore, in order to prevent the excessive division and proliferation of tumor cells, tubulin inhibitors have become an important class of anti-tumor therapeutic drugs. There are many kinds of antitumor drugs developed with it as the target, such as: colchicine, podophyllotoxin, vinblastine, paclitaxel, etc. These drugs effectively bind to tubulin in the active domain of tubulin, prevent the normal function of tubulin, and then prevent the growth of tumor cells and achieve the pu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/77A61K31/365A61P35/00A61P35/02
CPCC07B2200/07C07D307/77
Inventor 尹小英罗永明张媛媛乾康高书婷丁若雯
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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