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Water-soluble Pt(II) anticancer complexes using 3-acetoxy-1,1-cyclobutane dicarboxylic acid radical as leaving group

A complex and cancer technology, which is applied to compounds containing elements of group 8/9/10/18 of the periodic table, medical preparations containing active ingredients, antineoplastic drugs, etc., can solve problems such as cumulative poisoning, and achieve Less toxic and side effects, high anticancer activity, and high solubility

Inactive Publication Date: 2009-03-18
KUNMING INST OF PRECIOUS METALS +1
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  • Claims
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Problems solved by technology

Platinum is a trace metal element that is not necessary for the human body, and it is easy to produce cumulative poisoning in the human body, and the accumulation of drugs is often related to its water solubility

Method used

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  • Water-soluble Pt(II) anticancer complexes using 3-acetoxy-1,1-cyclobutane dicarboxylic acid radical as leaving group
  • Water-soluble Pt(II) anticancer complexes using 3-acetoxy-1,1-cyclobutane dicarboxylic acid radical as leaving group
  • Water-soluble Pt(II) anticancer complexes using 3-acetoxy-1,1-cyclobutane dicarboxylic acid radical as leaving group

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Embodiment Construction

[0013] (1) Preparation of 3-acetoxy-1,1-silver cyclobutane dicarboxylate

[0014] 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-hydroxyl 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, and recrystallize in isopropyl ether to obtain a white crystal , and dried at 60°C to obtain 15.5 g of 3-acetoxy-1,1-cyclobutanedicarboxylic acid, mp: 128-129°C, yield 60%.

[0015] Get 3-acetoxy-1,1-cyclobutanedicarboxylic acid 10g, be dissolved in the water of 100ml, adjust PH=6-7 with 1mol / LNaOH, add 104mmol, 100ml AgNO3 (excessive 5%), obtain 3- Silver precipitate of acetyloxy-1,1-cyclobutanedicarboxylate was collected by filtration, washed with water and ethanol, and dried under vacuum at 60-70°C for 4 hours ...

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Abstract

The invention relates to a novel water-soluble platinum (II) anticancer complex, a leaving group of which is 3-acetoxy-1 and 1-cyclobutane dicarboxylate root (3-COO-CBDCA), and a carrier of which is an ammonia / amine ligand of a listed platinum antitumor drug. The carrier comprises ammonia (NH3), 1R, 2R-diamino cyclohexane (DACH), 1,2-bis (aminomethyl)-cyclobutane, 2-isopropyl-(4R, 5R)-4, 5-bis (aminomethyl)-1 and 3-dioxo-cyclopentane. The novel water-soluble platinum (II) anticancer complex can be synthesized by the normal preparation method of the platinum antitumor drug. The antitumor activity of the complex is equivlent to that of the prior carboplatin frequently used in clinic, and the toxicity and side-effect of the complex are obviously less than those of carboplatin, can be made into freeze-dried powder or injection for cancer treatment in clinic.

Description

technical field [0001] The invention relates to a class of water-soluble platinum (II) anticancer complexes with 3-acetoxy-1,1-cyclobutane dicarboxylate as a leaving group, belonging to the field of chemical pharmacy. 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 disease. According to the estimates of the World Health Organization, in 2005, 7.6 million people died of cancer among the 58 million deaths in the world. It is estimated that 84 million people will die of cancer in the next 10 years. In recent years, due to factors such as environmental deterioration, bad living habits, and population aging, the incidence of cancer in my country has also been increasing. There are 2.2 million new cancer cases and 1.6 million cancer deaths each year. Therefore, cancer has become one of the medical problems that human beings urgently need to overcome. Curre...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/555A61P35/00
Inventor 刘伟平楼丽广谌喜珠侯树谦叶青松余尧
Owner KUNMING INST OF PRECIOUS METALS
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