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Anthraquinones tetracyclic compound having anticancer activity

A technology of compounds and quinones, applied in the application field of active ingredients of anticancer drugs, can solve problems such as poor water solubility and difficulty in injection preparations

Inactive Publication Date: 2008-07-23
TIANJIN HEMAY BIO TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that these compounds have poor water solubility, which has encountered great difficulties in the development of injection preparations

Method used

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  • Anthraquinones tetracyclic compound having anticancer activity
  • Anthraquinones tetracyclic compound having anticancer activity
  • Anthraquinones tetracyclic compound having anticancer activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0145] Boc-Diethylene glycol amine

[0146] Add 52.5 g (500 mmol) of diglycolamine and 200 ml of chloroform into a 1000 ml three-necked flask equipped with mechanical stirring, and cool down to 20° C. in an ice bath. 109g (500mmol) (Boc) 2 O was dissolved in 200ml of chloroform, added dropwise into the reaction flask with stirring, and stirred overnight at room temperature after dropping. After the reaction was completed, 400ml of water was added to the reaction solution, and the liquid was separated. The obtained organic phase was washed twice with water and twice with saturated brine, dried over anhydrous magnesium sulfate, filtered, spin-dried, and vacuum-dried to obtain 99.607g of compound I.

Embodiment 2

[0148] Boc-diethylene glycol amine p-toluenesulfonate

[0149] Add 99.607g of compound 1 and 102.0g of p-toluenesulfonyl chloride into a 500ml three-neck flask equipped with mechanical stirring, cool down to 15°C in an ice bath, drop 160ml of 20% NaOH aqueous solution, and stir overnight at room temperature. After the reaction was completed, the reaction solution was extracted three times with ethyl acetate, the organic phases were combined, washed once with saturated brine, dried over anhydrous magnesium sulfate, filtered and spin-dried to obtain 150.258 g of compound 2.

Embodiment 3

[0151] tert-Butoxycarbonyl-aminoethoxyethylphthalimide

[0152] 87.689g (244.2mmol) of compound 2, 67.766g (366.3mmol) of phthalimide potassium salt, and 150ml of anhydrous DMF were added to a 250ml single-necked flask, stirred at room temperature for 1 hr, and then stirred overnight at 55°C. After the reaction was completed, 2000ml of water was added to the reaction solution, extracted three times with ethyl acetate, the organic phases were combined, washed twice with water, once with 5% NaOH, twice with saturated saline, dried and filtered over anhydrous magnesium sulfate, and the solvent was spun off to obtain the product 62.192 g. 1 H NMR: δ7.831(m, 2H), δ7.702(m, 2H), δ4.915(s, 1H), δ4.099(t, 2H), δ3.866(t, 2H), δ3. 669(t, 2H), δ3.500(t, 2H), δ3.238(t, 2H), δ1.389(s, 9H)

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Abstract

The invention provides a tetracyclic anthraquinone with selective absorption and selective displacement, which is suitable for diseases that can be effectively treated by all tetracyclic anthraquinones, comprising but not limited to intestinal cancer, liver cancer, gastric cancer, breast cancer, lung cancer, ovarian cancer, prostate cancer, glioma, lymph cancer, skin cancer, melanoma, thyroid cancer, multiple myeloma and leukaemia.

Description

technical field [0001] The invention relates to anthraquinone tetracyclic compounds with anticancer activity, their preparation method and their application as active ingredients of anticancer drugs. technical background [0002] Cancer is one of the most important diseases that endanger human health, and its mortality rate ranks second in the world compared with other diseases. At present, cancer treatment includes comprehensive measures such as surgery, radiotherapy, chemotherapy, and immunotherapy. Gene therapy is still in the experimental research stage, and drug therapy is becoming more and more important in comprehensive treatment. means. More than 500,000 anticancer drugs have been screened worldwide, but only more than 70 kinds have been approved for marketing in various countries, and they have the disadvantages of insufficient selectivity and strong side effects. direction. [0003] Doxorubicin (Doxorubicin), epirubicin (Epirubicin) and daunorubicin (Daunorubici...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/244A61K31/704A61P35/00C07K5/04
CPCA61K31/704A61P35/00A61P43/00
Inventor 张和胜霍爱红李振重孙福亮
Owner TIANJIN HEMAY BIO TECH CO LTD
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