Monosilyl-containing platinum complex and application thereof

A technology of platinum complexes and monosilyl groups, which is applied in the field of platinum complexes containing monosilyl groups, can solve the problems of patients with kidney and nerve side effects, drug resistance, etc., and achieve reduction or elimination of repairing effects, elimination of repairing effects, and good curative effect Effect

Inactive Publication Date: 2019-11-08
湖南科因生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the disadvantages of the platinum complexes in the above-mentioned reports are that the patients will have side effects such as kidney nerves after drug treatment, and drug resistance will develop after use.

Method used

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  • Monosilyl-containing platinum complex and application thereof
  • Monosilyl-containing platinum complex and application thereof
  • Monosilyl-containing platinum complex and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Preparation of Compound 2 Potassium Trichloro-Amine Platinate (II) and Compound 3 Cis-Aminotrimethylsilylethylaminochloroiodoplatinum

[0036]

[0037] (1) Raw materials (1) cis-diaminodichloroplatinum (5.0g, 0.017mol), tetraethylammonium (3.57 g, 1.2 times the equivalent) were dissolved in 130mL dimethylacetamide, and inert gas protection , Heated at 105°C for 12 hours, then distilled the solution to 50mL under reduced pressure, added 300mL of cyclohexane and ethyl acetate (1:1), and kept the suspension at -12°C for 12 hours. The precipitated crystals were filtered and dried in vacuo to give the crude product as an orange solid. Add 50 mL of deionized water, stir at 25°C for 30 minutes, and then filter. The obtained filtrate was put into Dowex 50W-X8 hydrogen ion exchange resin and stirred for 1 hour, then the filtrate and solid resin were separated by filtration, and the filtrate was concentrated to 5 mL. At 0°C, 2 mL of saturated potassium chloride solution was ...

Embodiment 2

[0042] Preparation of compound 4 cis-aminotrimethylsilylethylaminodichloroplatinum

[0043]

[0044] (1) Compound 3 cis-aminotrimethylsilylethylaminochloroiodoplatinum (400 mg, 0.81 mmol) and silver nitrate (272 mg, 1.6 mmol) were dissolved in 4 mL of deionized water, and stirred at 22° C. in the dark for 6 hours. A small amount of activated charcoal was added and stirred for 30 minutes, then the solid was filtered. Then 1 mL of concentrated hydrochloric acid was added to the filtrate, and stirring was continued for 2 hours. The resulting yellow precipitate was filtered, the filter residue was rinsed with dimethyl ether, and vacuum-dried to obtain the pure product compound 4 cis-aminotrimethylsilylethylaminodichloroplatinum (315mg)

[0045] Compound 4 cis-aminotrimethylsilylethylaminodichloroplatinum: 195 Pt NMR (DMF-d 6 ): δ-2184 ppm; 1 HNMR (Aceton-d6 ):δ0.04ppm(s,9H,TMS),1.0(m,2H,CH 2 ),2.76(m,2H,CH 2 ),4.0(br,2H,NH 2 ),4.63(br,2H,NH 3 ).C 5 h 18 PtSiN 2 Cl 2...

Embodiment 3

[0047] Preparation of compound 5 cis-aminotrimethylsilylmethylaminochloroiodoplatinum

[0048]

[0049] At 0°C, dissolve 300 mg of the raw material compound 2 potassium trichloro-ammine platinum (II) in 4 mL of deionized water, add 240 mg of sodium iodide and 0.12 mL of 2-trimethylsilylethylamine, and keep this temperature for the reaction 4 hours. After the precipitate was filtered, the filter residue was washed with diethyl ether, and the filter residue was vacuum-dried to obtain a solid product compound 5 trimethylsilylmethylaminochloroiodoplatinum (290 mg).

[0050] Compound 5 Trimethylsilylaminochloroiodoplatinum: 195 Pt NMR (DMF-d 6 ): δ-2631ppm; 1 H NMR (DMF-d 6 ): δ0.11ppm(s,9H,TMS),2.36(m,2H,CH 2 ),4.2(br,2H,NH 2 ), 4.68(br,2H,NH 3 ).

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Abstract

The invention provides a monosilyl-containing platinum complex and application thereof. The structure of the complex is as shown in formula I, wherein X and Y are independently selected from halogen,hydroxyl, amino, a hydrated ion, -OC(O) R, acylamino or a sulfonic acid group separately; R is hydrogen, C1-4 alkyl or trimethylsilyl; or X and Y are connected with each other to form a dicarboxyl lactyl or a 1, 1'-cyclobutane dicarboxyl lactyl, wherein n can be a value of 1, 2, 3, or 4. The platinum complex molecule disclosed by the invention has high lipophilicity and is easy to migrate to tumorcells to achieve a therapeutic effect; hydrogen bond stability is formed between the platinum complex and DNA, the platinum complex and DNA or RNA form a compound, so that cell synthesis, transcription or replication is interfered and even prevented, and an effect of inhibiting or killing cancer cells is achieved; compared with another platinum complex, the platinum complex has a better curativeeffect, and a way is provided for overcoming the drug resistance of cisplatin and relieving or eliminating neurotoxic side effects of patients; and the antitumor effect of the monosilyl-containing platinum complex is better than the antitumor effect of other like drugs.

Description

technical field [0001] The invention belongs to the technical field of platinum complexes; more specifically, it relates to a platinum complex containing a monosilyl group and its application. Background technique [0002] As a difficult problem in the field of human medicine, cancer has seriously threatened human life and health for many years. More than 7 million people die from cancer every year in the world. Countries around the world invest a lot of scientific research funds and manpower in the research and development of anticancer drugs every year, and platinum complexes are one of the results. [0003] For a long time, platinum complexes have been widely used in the field of cancer therapy. As early as the 1960s, the structure of cisplatin was found to have anti-tumor properties, and since then people have begun to conduct extensive research on the structure of cisplatin. At present, thousands of platinum complex derivatives have been developed for pharmaceutical ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0093
Inventor 肖泽军尹迪
Owner 湖南科因生物科技有限公司
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