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Anticancer compounds and their applications

A compound, cancer technology, applied in the direction of steroids, silicon compounds, active ingredients, antitumor drugs, etc., can solve rare problems and achieve the effect of no toxic side effects

Active Publication Date: 2017-03-01
DM INTELLIGENCE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Anticancer compounds that regulate tumor cell growth and angiogenesis by regulating the Rho / Rho kinase signaling pathway are still rare

Method used

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  • Anticancer compounds and their applications
  • Anticancer compounds and their applications
  • Anticancer compounds and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Embodiment 1: the synthesis of lanosterol derivative

[0085] (1) Dissolve 5 grams of lanosterol in 20 milliliters of pyridine. After complete dissolution, add 2 milliliters of acetic anhydride (about 2 equivalents) dropwise, and react at room temperature for 12 hours to end the reaction. The reaction mixture was concentrated under reduced pressure, and the concentrate was cooled with an ice bath, and a 10% aqueous solution of sodium bicarbonate was slowly added dropwise until no bubbles emerged completely, extracted three times with ethyl acetate, and the organic layers were combined. The organic layer was washed with saturated aqueous sodium chloride solution, dried with anhydrous sodium sulfate, filtered, and the organic layer was spin-dried to obtain 5.5 grams of crude product. After column separation, 4.5 grams of the target product were obtained as a white solid with a yield of 84 %. MS(ESI): m / z569[M+H + ]; the hydrogen spectrum measured by the target product i...

Embodiment 2

[0103] Embodiment 2: the synthesis of lanosterol derivative

[0104] Dissolve 0.1 g of LD020 in 10 ml of dichloromethane, add 80 mg (about 3 equivalents) of m-chloroperoxybenzoic acid under vigorous stirring, and react at 0°C for 10 hours. Add 0.1 g of calcium hydroxide, stir at room temperature for 1 hour, filter out the solid, wash the solid with 50 ml of dichloromethane, combine the filtrates, concentrate to obtain crude products, and separate on the column to obtain 20 mg of the following LD026-1 respectively The product (yield 18%) and 30 mg of the following product No. LD026-2 (yield 28%) were both white solids. The hydrogen spectrum shows that the hydrogen spectrum of LD026-1 and LD026-2 is the same as that of compound LD020 Figure 1 Sample. Product No. LD026-1 MS(ESI): m / z485[M+H + ], LD026-2 product MS (ESI): m / z 501 [M+H + ]. The reaction equation is as follows:

[0105]

Embodiment 3

[0106] Embodiment 3: the synthesis of lanosterol derivative

[0107] Dissolve 0.1 g of LD021 in 10 ml of dichloromethane, add 40 mg (about 1.5 equivalents) of m-chloroperoxybenzoic acid under vigorous stirring, and react at 0°C for 10 hours. Add 0.1 g of calcium hydroxide and stir at room temperature for 1 hour. The solid was filtered out, and the solid was washed with 50 ml of dichloromethane. The filtrates were combined and concentrated to obtain a crude product, which was separated on a column to obtain 10 mg of the target product with a yield of 10% as a white solid. Proton spectra showed that LD0027 had the same spectrum as compound LD021. MS(ESI): m / z519[M+H + ]. The reaction equation is as follows:

[0108]

[0109] In order to illustrate the technical scheme of the present invention, the compound number is LD027.

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Abstract

The invention relates to an anticancer medicine which is a lanosterol derivative. The compound has an anticancer effect, and can inhibit the growths of lung cancer cells, liver cells, mammary gland cells, brain cancer cells, and pancreatic cancer cells. The medicine is a compound with a general formula of (I), (II), (III), or (IV). The invention also provides an application of the compound or pharmaceutically acceptable salt thereof in preparing medicines used for treating cancers. The medicine can be used independently, and can be used in combination. Especially, the medicine can be used in combination with gemcitabine or nexavar. The medicine can be used in treating cancers such as lung cancer, liver cancer, pancreatic cancer, breast cancer, brain cancer, and the like.

Description

technical field [0001] The invention relates to an anticancer compound, in particular to a lanosterol derivative and its application in the preparation of medicines for treating cancer. Background technique [0002] Cancer is a general term for various malignant tumors in which cells grow and divide faster than normal cells and can invade primary tissue or spread to other sites. Cancer is currently treated mainly through surgery, radiation therapy, chemotherapy and immunotherapy. However, surgical therapy cannot completely remove extensive metastases; radiotherapy cannot selectively deliver radiation to cancer cells; chemotherapy cannot selectively kill cancer cells in the presence of rapidly proliferating normal cells; immunotherapy is mostly limited to the use of Cytokines or therapeutic cancer vaccines, the use of cytokines for therapy is limited by life-threatening toxicity, and the use of cancer vaccines often develops immune tolerance over time. [0003] Therefore, o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/695A61K31/58A61P35/00
Inventor 谢伟东刘昕
Owner DM INTELLIGENCE LTD
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