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Antitumor compound, its preparation method and application

A technology for anti-tumor drugs and compounds, applied in the field of medicine, can solve the problems of obvious adverse reactions, affecting the quality of life of patients, and poor selectivity of cytotoxic drugs.

Inactive Publication Date: 2014-07-09
HUAZHONG UNIV OF SCI & TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] (2) Adverse reactions: Chemotherapy, as the main treatment for malignant tumors, has strong lethality and quick results, but its adverse reactions are also obvious, especially the selectivity of cytotoxic drugs is not strong, while inhibiting or killing tumor cells, It also causes varying degrees of damage to normal cells and tissues of the human body.
These adverse reactions not only directly affect the quality of life of patients, but also hinder the smooth implementation of chemotherapy regimens.

Method used

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  • Antitumor compound, its preparation method and application
  • Antitumor compound, its preparation method and application
  • Antitumor compound, its preparation method and application

Examples

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Effect test

Embodiment 1

[0099] Preparation of 2-(1-hydroxy-4-one-2,5-cyclohexadiene)-pyran-4-one

[0100] (1) 2-(2-bromoethyl)-1,3-dioxolane and sodium nitrite were nitrated and purified to obtain a yellow liquid substance. The specific operation is as follows: 1 equivalent of 2- (2-Bromoethyl)-1,3-dioxolane, 1.3 equivalents of sodium nitrite, and 0.5 equivalents of phloroglucinol were dissolved in DMSO, mixed uniformly, and reacted at room temperature for 18 hours. The reaction mixture was dispersed in water, extracted twice with an equal volume of dichloromethane, the dichloromethane layer was taken, and the solvent was recovered at 70°C. The product was developed in an iodine tank under TLC conditions with a volume ratio of petroleum ether / acetone of 10:1, and the Rf value was 0.3. Using petroleum ether / acetone with a volume ratio of 10:1 as normal phase silica gel for column chromatography purification to obtain a yellow liquid product, which is judged to be 2-(2-nitroethyl)-1,3- Dioxolane [See...

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Abstract

The invention discloses an antitumor compound 2-(1-hydroxy-4-ketone-2, 5-cyclohexadiene)-pyran-4-ketone, its preparation method and an application. The antitumor compound has structural features as shown in the formula 1. The compound has a structure of alpha, beta-nonsaturated ketone, and has a remarkable effect of inhibiting human gynecologic tumor, prostatic neoplasms, digestive system neoplasms and hematological malignancy without influencing a normal hematopoietic system and a metabolic system. In addition, the compound can effectively inhibit the tumor growth of mice bearing H22 tumor but has no influence on the ratio of peripheral white blood cell to peripheral blood granulocyte to lymphocyte, marrow nucleated cells, the ratio of marrow granulocyte series to erythrocyte series, thymus index and spleen index. The synthetic method of the compound is as follows: the antitumor compound is synthesized by six-step reactions with 2-(2-bromomethyl)-1, 3-dioxolane as a raw material.

Description

technical field [0001] The invention belongs to the field of medicine and relates to antitumor drugs, in particular to drugs for treating mammalian gynecological tumors, prostate tumors, digestive system tumors, blood system tumors and metabolic system tumors. Background technique [0002] Malignant tumors seriously threaten human life. According to the results of the third national resident cause of death survey, the death rate caused by tumors in my country ranks second among all causes, accounting for 17.9%, and the incidence rate is increasing year by year. In the past 20 years, the mortality rate of cancer in my country has increased by 29.42%. Among middle-aged and middle-aged people, tumors have ranked first among all causes of death. Finding effective anti-cancer drugs and methods to completely conquer cancer is an important topic in the world's medical research. [0003] Chemotherapy plays a pivotal role in the research of cancer treatment. Most of the existing ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D309/38A61K31/351A61P35/00
Inventor 阮金兰袁倩颖熊朝梅刘子维
Owner HUAZHONG UNIV OF SCI & TECH
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