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Water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex

An anti-tumor, water-soluble technology, applied in the direction of anti-tumor drugs, active ingredients of heavy metal compounds, compounds containing Group 8/9/10/18 elements of the periodic table, etc. Big side effects etc.

Inactive Publication Date: 2010-07-28
KUNMING INST OF PRECIOUS METALS +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Recent clinical studies have found that although they have high activity in vitro, their curative effect in vivo is not good, and their toxicity and side effects are large, so the prospect is not optimistic.

Method used

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  • Water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex
  • Water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex
  • Water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex

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Experimental program
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Effect test

Embodiment Construction

[0014] (1) Preparation of 3-acetoxy-1,1-silver cyclobutane dicarboxylate

[0015] Firstly, 3-hydroxy-1,1-cyclobutane dicarboxylic acid (mp 151-152° C.) was prepared according to the method reported in the literature [Inorganica Chimica Acta, 2004, 357, 4452-4466]. Take 20g of 3-hydroxy-1,1-cyclobutanedicarboxylic acid, dissolve it in 200ml of acetone, add 33g of freshly distilled acetyl chloride, stir at 50°C for 4h, evaporate the solvent to obtain a crude product, recrystallize in isopropyl ether to get White crystals were dried at 60°C to obtain 15.5 g of 3-acetoxy-1,1-cyclobutanedicarboxylic acid, mp: 128-129°C, yield 60%.

[0016] Take 10g of 3-acetoxy-1,1-cyclobutanedicarboxylic acid, dissolve it in 100ml of water, and use 1mol / L NaHCO 3 Regulate PH=5-6, add 104mmol, 100ml AgNO3 (excessive 5%), obtain 3-acetoxy-1,1-silver precipitate of cyclobutane dicarboxylate, collect by filtration, after washing with water, ethanol, in 60-70 After vacuum drying at °C for 4 hours, 19...

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Abstract

The invention discloses a water-soluble carboxyl-bridge dicaryon Pt (II) anti-tumor complex, which has a chemical name of cis-tetrammine-miu-di (3-acetoxy-1, 1-cyclobutane dicarboxylate-O1, O2) dicaryon platinum (II), and can be synthesized by adopting the method preparing the conventional platinum based anti-cancer drug. The anticancer activity of the complex of the invention is higher than the platinum based drug of carboplatin commonly used in clinic, the toxic side effect of the invention is significantly lower than the toxic side effect of carboplatin, and the invention can be made into lyophilized powder or injecta to be used in the clinical cancer treatment.

Description

technical field [0001] The invention relates to a novel water-soluble carboxybridge dinuclear platinum (II) anticancer complex, which belongs to the field of chemical pharmacy. Background technique [0002] Malignant tumor is a disease that seriously threatens human health and life, and is the second leading cause of death in the world after cardiovascular disease. Chemotherapy is one of the important means of clinical treatment of malignant tumors. The basis of chemotherapy is chemical drugs. Therefore, countries around the world invest a lot of manpower and material resources in the research and development of anti-tumor drugs every year. Platinum anticancer drugs are a class of inorganic anticancer compounds developed in the late 1970s. Due to their strong anticancer activity, wide spectrum of action, and unique mechanism of action, they do not produce cross-resistance with non-platinum anticancer drugs. , is currently the drug of choice for the treatment of many malign...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/282A61K9/19A61K9/08A61P35/00
Inventor 刘伟平楼丽广谢明进谌喜珠叶青松余尧常桥稳侯树谦
Owner KUNMING INST OF PRECIOUS METALS
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