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Platinum (IV) anticancer compounds with dihydrogen phosphate radical as axial ligand

A dihydrogen phosphate compound technology, applied in the field of biopharmaceuticals, can solve problems such as poor water solubility, poor anticancer activity, and failure to be approved for marketing, and achieve good selectivity, high anticancer activity, and good clinical application prospects.

Active Publication Date: 2016-04-13
KUNMING INST OF PRECIOUS METALS +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Satraplatin has been in clinical trials for 17 years, but has not been approved for marketing
The main reasons include the poor water solubility of these compounds (≈1 mg / ml), non-targetability, and inferior anticancer activity to cisplatin, carboplatin, and oxaliplatin

Method used

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  • Platinum (IV) anticancer compounds with dihydrogen phosphate radical as axial ligand
  • Platinum (IV) anticancer compounds with dihydrogen phosphate radical as axial ligand
  • Platinum (IV) anticancer compounds with dihydrogen phosphate radical as axial ligand

Examples

Experimental program
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Embodiment Construction

[0041] (1) The synthetic method of Pt (IV) anticancer compound PPt1 of the present invention

[0042] Weigh 8.40g (28mmol) cisplatin, add 250ml of water, stir, heat to 60°C, add 30wt% H 2 o 2 420ml, continue to stir and react at 60°C for 4 hours, cool to room temperature, precipitate a light yellow product, filter, wash with ice water, dry, and recrystallize in water to obtain light yellow crystals of cis, trans, cis-[ Pt(IV)(NH 3 ) 2 (OH) 2 Cl 2 ]5.8g, the yield is about 62%.

[0043] Accurately weigh 2.061g (6.17mmol) cis, trans, cis-[Pt(IV)(NH 3 ) 2 (OH) 2 Cl 2 ], add 0.678 grams of 85% phosphoric acid solution (5.88mmol, be equivalent to 95% of stoichiometry), after stirring and mixing, add 50ml of water stirring reaction again at 60 ℃ and after concentrating under reduced pressure to near dryness, add 100ml of Stir to dissolve in water, cool to room temperature, filter out unreacted cis, trans, cis-[Pt(IV)(NH 3 ) 2 (OH) 2 Cl 2 ], the filtrate was freeze-drie...

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Abstract

The invention relates to platinum (IV) anticancer compounds with a dihydrogen phosphate radical as an axial ligand. The chemical structure of the compounds is shown in the description. In the structure, a carrier group 2A is an ammonia / amine liand, and comprises 2NH3, 1R,2R-cyclohexanediamin, 1,2-bis(aminomethyl)cyclobutane, NH3 / cyclopentamine and NH3 / cyclohexylamine; and leaving groups 2X are the leaving groups of platinum (II) anticancer compounds existing at present, and comprise 2Cl<->, an oxalate radical, a 1,1-cyclobutanedicarboxylate radical and a propane dicarboxylate radical. Phosphoric acid bonding is helpful for running of compounds to cancer cell nuclei, improving the selectivity of cancer cells, and makes the compounds mediate compound targeting osteocarcinoma and have very strong anticancer effect. The compounds have the advantages of good water solubility and stability, and are highly suitable for being used as anticancer drugs.

Description

technical field [0001] The invention relates to a class of Pt (IV) compounds with dihydrogen phosphate as axial ligands and their use as anticancer drugs, belonging to the field of biopharmaceuticals. Background technique [0002] Platinum drugs are a very important class of anticancer drugs, widely used in clinical treatment of common multiple malignant tumors [1] . According to the latest statistics, currently 70% of clinical combined chemotherapy regimens are based on platinum drugs or participate in compatibility. [2] . The currently approved platinum drugs mainly include Cisplatin, Carboplatin, Nedaplatin, Oxaliplatin, Heptaplatin and Lobaplatin. [3,4] , among them, cisplatin, carboplatin and oxaliplatin (structural formula 1) are considered to be representatives of platinum anticancer drugs, and have been included in the pharmacopoeias of most countries and regions such as the United States, Japan, the European Union, and China. widely used clinically. [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00A61P35/04
CPCC07F15/0093
Inventor 刘伟平楼丽广侯树谦高安丽谢成英全海天姜婧
Owner KUNMING INST OF PRECIOUS METALS
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