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Platinum (II) complexes having antitumor activities, and preparation methods thereof

A technology of anti-tumor activity and complexes, applied in the field of medicine, can solve problems such as narrow anti-cancer spectrum, large toxic and side effects, and bone marrow suppression

Inactive Publication Date: 2013-06-05
KUNMING GUIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drugs currently on the market also have many inherent shortcomings: large toxic and side effects, can cause nausea, vomiting, bone marrow suppression, etc., cross-resistance between each other, and narrow anti-cancer spectrum, etc. These shortcomings limit their wider application. use

Method used

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  • Platinum (II) complexes having antitumor activities, and preparation methods thereof
  • Platinum (II) complexes having antitumor activities, and preparation methods thereof
  • Platinum (II) complexes having antitumor activities, and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Weigh 4.8g of iodoplatinum with water and stir it into a suspension, place it on a constant temperature magnetic stirrer, weigh 3.4g of silver nitrate dissolved in water and add it to the suspension of iodoplatinum, stir and react at 55°C for 4h, After the AgI precipitate was removed by filtration, a light yellow transparent solution was obtained. The light yellow transparent solution was placed on a constant temperature magnetic stirrer and heated to 60°C. Weighed 1.8g of sodium methylmalonate dissolved in water and added dropwise to the above light yellow transparent solution. After reacting for 1 hour, the obtained precipitate was filtered and dried. 1.9 g of off-white crystalline powder was obtained, yield: 55.1%. Recrystallize with boiling water and dry to obtain 0.5 g of white crystalline powder, yield: 26.3%.

Embodiment 2

[0019] Example 2: Weigh 4.8g of iodoplatinum with water and stir it into a suspension, place it on a constant temperature magnetic stirrer, weigh 3.4g of silver nitrate dissolved in water and add it to the suspension of iodoplatinum, stir and react at 60°C for 4h, After the AgI precipitate was removed by filtration, a light yellow transparent solution was obtained. The light yellow transparent solution was placed on a constant temperature magnetic stirrer and heated to 60°C. Weighed 1.8g of sodium methylmalonate dissolved in water and added dropwise to the above light yellow transparent solution. After reacting for 1 hour, the obtained precipitate was filtered and dried. 2.1 g of off-white crystalline powder was obtained, yield: 61.8%. Recrystallized with boiling water and dried to obtain 0.7 g of white crystalline powder, yield: 33.3%.

Embodiment 3

[0020] Example 3: Weigh 4.8g of iodoplatinum with water and stir it into a suspension, place it on a constant temperature magnetic stirrer, weigh 3.4g of silver nitrate dissolved in water and add it to the suspension of iodoplatinum, stir and react at 65°C for 4h, After the AgI precipitate was removed by filtration, a light yellow transparent solution was obtained. The light yellow transparent solution was placed on a constant temperature magnetic stirrer and heated to 60°C. Weighed 1.8g of sodium methylmalonate dissolved in water and added dropwise to the above light yellow transparent solution. After reacting for 1 hour, the obtained precipitate was filtered and dried. 2.0 g of off-white crystalline powder was obtained, yield: 58.0%. Recrystallized with boiling water and dried to obtain 0.7 g of white crystalline powder, yield: 35.0%.

[0021] 2. Preparation of cis-ethylmalonate-diammine platinum (II)

[0022] Example 1: Weigh 4.8g of iodoplatinum with water and stir it in...

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Abstract

The invention relates to platinum (II) complexes having antitumor activities, and preparation methods thereof. The platinum (II) complexes treat an ammonia molecule as an accompanying group, and treat methylmalonic acid and ethylmalonic acid as leaving groups respectively. The series of the above compounds have the antitumor activities. The structure of the compounds is shown in the specification.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a platinum complex, which has antitumor activity. Background technique [0002] Cancer is a disease that seriously threatens human health and life, and is the second leading cause of death in the world after cardiovascular and cerebrovascular diseases. In recent years, due to environmental deterioration, bad living habits and population aging and other factors, the incidence of cancer in my country has been increasing. Cancer has become one of the medical problems that human beings urgently need to overcome. [0003] In the 1960s, Rosenberg, a professor at Michigan State University in the United States, discovered that cisplatin has anticancer activity when studying the effect of DC electric field on the growth of Escherichia coli, and through clinical verification, cisplatin has good therapeutic effects on various tumors , thus opening up a new field of research on the anticanc...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/282A61P35/00
Inventor 朱泽兵普绍平何键李永年王庆琨丛艳伟李学杰
Owner KUNMING GUIYAN PHARMA
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