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Platinum complexes of quercetin and derivatives thereof, as well as preparation and use thereof

A technology of quercetin and complexes, which is applied in the field of complexes of quercetin or its derivatives with platinum and its salts, and can solve problems such as poor solubility, drug resistance, and high toxicity

Inactive Publication Date: 2009-07-08
BEIJING JIASHILIANBO PHARM SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]However, current platinum-based antineoplastic drugs have relatively high toxicity, such as bone marrow suppression, kidney toxicity, nerve damage, etc., poor solubility, relatively narrow anticancer spectrum, and There are disadvantages such as drug resistance

Method used

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  • Platinum complexes of quercetin and derivatives thereof, as well as preparation and use thereof
  • Platinum complexes of quercetin and derivatives thereof, as well as preparation and use thereof
  • Platinum complexes of quercetin and derivatives thereof, as well as preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Get potassium chloroplatinite 20g (48mmol) and add water 1000ml and stir and dissolve in a three-necked flask, weigh potassium iodide 47g (283mmol) and drop into the reaction solution, and react for 2 hours under nitrogen protection and dark room temperature to obtain a black solution (iodoplatinous acid Potassium). Take 16ml of ammonia water (120mmol) with a concentration of 7.5mmol / ml, continue to react at room temperature in the dark for 2 hours, filter, wash with water (30ml×2 times), ethanol (30ml×2 times), diethyl ether (30ml×2 times), and pump Dry to yellow powder, that is, diiododiammine platinum Pt(NH 3 ) 2 I 2 A total of 21.1 g, yield 93.4%.

Embodiment 2

[0066] [Example 2] [Pt(NH 3 ) 2 (H 2 O) 2 ](NO 3 ) 2

[0067] Get 8.16g (48mmol) of silver nitrate and 240ml of pure water and drop into a 500ml eggplant bottle and stir, add a total of 11.592g (24mmol) of diiododiammine platinum prepared in Example 1, pass into nitrogen protection, avoid light, and react at room temperature for 24 hours . The silver iodide precipitate was filtered off, and washed with water (20ml×3 times) to obtain [Pt(NH 3 ) 2 (H 2 O) 2 ](NO 3 ) 2 Colorless transparent filtrate.

Embodiment 3

[0068] [Example 3] Preparation of quercetin and ammine platinum (II)

[0069] Get the diiododiammine platinum 12.5g (26mmol) that embodiment 1 prepares, add 9.3g AgNO 3 (55mmol)AgNO 3 solution, filtered to remove AgI. Add 7.9g (26mmol) quercetin to the filtrate, avoid light and stir at 60±5°C for 35 hours, filter the reaction mixture through a layer of silica gel to obtain a solution, concentrate under reduced pressure to 150ml, filter to obtain a brown-black solid, wash with a small amount of water , protected from light and air-dried to obtain 10.9 g of quercetin and ammine platinum, with a yield of 78%.

[0070] IR 3422(NH), 1656(C=O), 569(Pt-O)

[0071] Elemental analysis Theoretical value: C (%) 34.03; H (%) 2.65; N (%) 5.29

[0072] Measured value: C (%) 34.27; H (%) 2.52; N (%) 5.01

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Abstract

The invention discloses quercetin or quercetin derivative and platinum complexes and salts thereof in the filed of medicines. The chemical structural formula of the complexes is the formula (I) or formula (II). The invention also discloses methods for preparing the complexes and the salts thereof and uses of the complexes and the salts thereof in the preparation of drugs for treating cancers.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically, it is a new class of complexes of quercetin or its derivatives and platinum and salts thereof with medical value, including its preparation method and application. Background technique [0002] Cancer (malignant tumor) is one of the most important diseases threatening human life at present. Statistics released by the World Health Organization show that since 1996, more than 10.3 million cancer patients have been newly diagnosed in the world every year. By the end of 1999, the total number of cancer patients in the world has exceeded 40 million. In 2001, the morbidity and mortality of cancer in the world increased by 22% compared with 1990, and it is the second leading cause of death after cardiovascular disease. According to the survey results released by the Ministry of Health of my country, the number of cancer patients in China has reached about 2.865 million, and there are abo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00C07D311/30A61K31/555A61P35/00
Inventor 陈小平阎亚矢丁浩
Owner BEIJING JIASHILIANBO PHARM SCI & TECH
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