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Application of composition containing cyclopenteno Cyclopenteno multi-hydrogen phenanthrene derivative in preparation of anti-tumor drug

A kind of technology of cyclopentene and derivatives, applied in the field of preparing medicines for anti-tumor

Inactive Publication Date: 2020-09-11
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the antitumor activity of compound II needs to be further improved.

Method used

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  • Application of composition containing cyclopenteno Cyclopenteno multi-hydrogen phenanthrene derivative in preparation of anti-tumor drug
  • Application of composition containing cyclopenteno Cyclopenteno multi-hydrogen phenanthrene derivative in preparation of anti-tumor drug
  • Application of composition containing cyclopenteno Cyclopenteno multi-hydrogen phenanthrene derivative in preparation of anti-tumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1 Oral solid preparation of a composition containing cyclopentene polyhydrophenanthrene derivatives and its preparation method

[0076] prescription

[0077]

[0078]

[0079]

[0080] Preparation

[0081] Take the prescribed amount of MIX (X-Y) and auxiliary materials, and pass through a 100-mesh sieve. Get MIX (X-Y), lactose, microcrystalline cellulose, crospovidone and starch and fully mix; get the prescription amount of hypromellose, and prepare a solution with a concentration of 10% based on hypromellose, Use lactic acid to adjust the pH to 3.0-4.0, add it to the above-mentioned mixture to make a soft material, granulate with a 16-mesh sieve, and dry at 80°C for 3-4 hours. Use a 16-mesh sieve to sieve the granules, add the prescribed amount of micropowder silica gel and magnesium stearate, mix well, fill the capsules, and each capsule weighs about 500mg;

[0082] Take the prescribed amount of MIX (X-Y) and auxiliary materials, and pass throu...

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Abstract

The invention provides an application of a composition containing a first cyclopenteno multi-hydrogen phenanthrene derivative and a second cyclopenteno multi-hydrogen phenanthrene derivative which aredifferent from each other in preparation of an anti-tumor drug. The specific definition of the cyclopenteno multi-hydrogen phenanthrene derivative is shown in the specification, and the tumor is preferably selected from one of prostate cancer, gastric cancer and esophageal cancer. The inhibition effect of the composition on proliferation of various tumor cells is obviously superior to that of anin-vivo active component compound II of a compound I on the market.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the use of a composition containing cyclopentenophenanthrene derivatives in the preparation of antitumor drugs. Background technique [0002] Compound I with the following structural formula is a cyclopentene polyhydrophenanthrene compound approved by the FDA for the treatment of castration-resistant prostate cancer and castration-sensitive prostate cancer. The research results of Yun-Kai Shi et al. confirmed (Eur JMed Chem.2018Feb 10; 145:11-22.), the in vivo active form of compound Ⅱ, compound Ⅱ, is sensitive to castration-resistant prostate cancer cell line PC-3 and castration IC of prostate cancer cell line LNCaP 50 They were about 2080 μg / L and 1150 μg / L, respectively. In the same study, Yun-Kai Shi et al. also disclosed the anti-proliferation activity of compound II on human esophageal cancer cell EC-109 and human gastric cancer cell MGC-803. Its IC 50 They ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/57A61K31/568A61K31/5685A61K31/573A61K31/58A61K31/566A61K31/567A61P35/00
CPCA61K31/566A61K31/567A61K31/568A61K31/5685A61K31/57A61K31/573A61K31/58A61P35/00A61K2300/00
Inventor 向飞梁乐
Owner 黄泳华
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