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Preparation method for metallic thiophene ring ternary complex with anti-cancer activity and application thereof

A technology of ternary complexes and anti-cancer activity, which can be used in medical preparations containing active ingredients, organic active ingredients, copper organic compounds, etc. The problem is to achieve the effects of significant apoptosis of promyelocytic leukemia cancer cells, strong anti-cancer ability and simple preparation method.

Inactive Publication Date: 2009-09-02
SHANGHAI NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The purpose of the invention is to provide a metallothiophene ring ternary complex with anticancer activity and its preparation method and application, so as to overcome the preparation method that most of the existing complexes are of conventional particle size and rarely have nanometer particle size. Moreover, the preparation method is complex and overcomes the defects of existing anticancer compounds such as high price, large dosage, high toxicity, large side effects, and easy pollution to the environment

Method used

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  • Preparation method for metallic thiophene ring ternary complex with anti-cancer activity and application thereof
  • Preparation method for metallic thiophene ring ternary complex with anti-cancer activity and application thereof
  • Preparation method for metallic thiophene ring ternary complex with anti-cancer activity and application thereof

Examples

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Embodiment 1

[0033] Weigh 0.666g (3mmol) of 2-thienoyltrifluoroacetone (HTTA) and dissolve it in 10ml of alcohol solvent, then add 3ml of 1mol / L sodium hydroxide solution, heat and stir; when the temperature rises to 60~65℃ , add dropwise 1mmol of rare earth chloride (by RE in advance 2 o 3 reacted with hydrochloric acid), stirred for 0.5-2h, then added dropwise 1mmol L of alcohol solution; after reacting for 4-8 hours, rotary evaporated, cooled, suction filtered, washed 2-4 times to obtain RE(TTA) 3 L·nH 2 O (n=1-7), vacuum-dried for 4-5 hours and then sealed and stored.

[0034] In the above method, HTTA is 2-thienoyltrifluoroacetone, and L is (R 1 =OH, Cl, Br, NH 2 Wait, R 2 =COOH, COONa etc.), RE can be La 3+ 、Ce 3+ 、Pr 3+ 、Nd 3+ 、Pm 3+ 、Sm 3+ 、Eu 3+ 、Gd 3+ , Tb 3+ 、Dy 3+ 、Ho 3+ , Y 3+ 、Er 3+ 、Tm 3+ and Yb 3+ One of them can also be a combination of more than one, such as rare earth La 3+ and Ce 3+ 、Pr 3+ and Nd 3+ 、Nd 3+ and Sm 3+ 、Eu 3+ and Er 3+ , even ...

Embodiment 2

[0040] Weigh 0.666g (3mmol) of 2-thienoyltrifluoroacetone (HTTA) and dissolve it in 20ml of alcohol solvent, then add 3ml of 1mol / L sodium hydroxide solution, heat and stir; when the temperature rises to 60-80 ℃, add dropwise 1mmolMtCl 2 After stirring for 0.5-2h, 1 mmol L of alcohol solution was added dropwise; after reacting for 6-8 hours, rotary evaporation, cooling, and washing were performed to obtain Mt 2 (TTA) 3 L·Cl 4 , vacuum-dried for 4 to 6 hours and then airtightly stored.

[0041] In the above-mentioned method, HTTA is thienoyl trifluoroacetone, and L is (R 1 =OH, CI, Br, NH 2 Wait, R 2 =COOH, COONa, etc.), Mt is Cu 2+ , Zn 2+ , Fe 3+ and other metal ions.

[0042] In the same way, the above-mentioned method can also be used to prepare thienoyltrifluoroacetone derivatives and the like with different rare earth ions and different (R 1 =OH, Cl, Br, NH 2 Wait, R 2 =COOH, COONa, etc.), as long as the specific method is to replace thienoyl trifluoroacet...

Embodiment 3

[0045] The complexes prepared in Examples 1 and 2 were respectively dissolved in dimethyl sulfoxide (DMSO), and prepared into solutions respectively, with a final concentration of 0.1 ng / mL, 1 ng / mL, 5 ng / mL, 10 ng / mL, 50 ng / mL mL was added to the culture medium of promyelocytic leukemia cells in the rapid growth phase, so that the final concentration of cells was 2×10 5 A / mL or so. After 48 hours, the cell growth was observed and counted under a fluorescent inverted microscope, and the results were as follows: Figure 4 shown.

[0046] Figure 5 Inhibition percentage of the ternary complex and its ligands prepared in Example 1 on the growth cycle of promyelocytic leukemia tumor cells.

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Abstract

The invention discloses a metallic thiophene ring ternary complex with anti-cancer activity. The complex has a chemical formula: RE(TTA)3L.nH2O(n=1-7) or Mt2(TTA)3L.Cl4. The complex has good chemical stability and thermal stability and can be used, stored and transported at a normal temperature. The ternary complex is 0.005 to 0.5 mu g / ml for the IC50 of a promyelocytic leukemia tumor cell, has a nanometer grade grain size range, and more easily enters and kills the cancer cell. In addition, the preparation method is simple, and has low preparation price, and little impact on the environment in a manufacturing link. The ternary complex has high biological availability and little dosage, and brings about less drug toxicity.

Description

technical field [0001] The invention relates to a preparation method of a ternary complex formed by a metal, an aromatic carboxylate or an aromatic carboxylate having a substituent at the para-position, and thienoyltrifluoroacetone, and its application in antitumor activity. Background technique [0002] Public health is the cause of disease prevention and health promotion for all members of the society. The death rate of cancer in our country remains high, so cancer experts regard cancer as the number one public enemy of public health in China: "If the government does not take effective measures now, the cancer death rate will double in the next 20 years, reaching 3 million." At the same time Cancer has always been a major disease that the whole world is trying to overcome. Cancer has not been effectively controlled so far, and it has become a major problem that threatens the survival of human beings. For this reason, the World Health Organization (WHO) predicts that cance...

Claims

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Application Information

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IPC IPC(8): C07F5/00C07F1/08C07F3/06C07F15/02C07D333/22A61K31/381A61K31/192A61P35/00
Inventor 许东芳何其庄沈智慧夏庆春杨自芳施阳
Owner SHANGHAI NORMAL UNIVERSITY
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