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5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound and preparation method and application thereof

A compound and drug technology, which is applied in the field of 5,5,6-polycyclic tetramacid-containing macrolactam compounds, can solve the problems of liver discomfort, large side effects and toxic effects, and poor chemotherapeutic drug selectivity.

Active Publication Date: 2018-10-09
OCEAN UNIV OF CHINA
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Problems solved by technology

Chemotherapy is a treatment method that uses chemical drugs to kill tumor cells, inhibit the growth and reproduction of tumor cells, and promote the differentiation of tumor cells. Almost all chemotherapy drugs can cause liver function damage, and abnormal liver function may occur in mild cases. Discomfort in the liver area occurs, and even can lead to toxic hepatitis; high doses of some chemotherapy drugs can cause renal function damage, resulting in low back pain, discomfort in the kidney area, etc., and due to the poor selectivity of chemotherapy drugs, while killing tumor cells, Normal cells and immune cells are also killed in large quantities, and the side effects and toxic effects are extremely great

Method used

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  • 5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound and preparation method and application thereof
  • 5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound and preparation method and application thereof
  • 5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound and preparation method and application thereof

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preparation example

[0050]

[0051] (1) Preparation of compound 1-6

[0052] Fermentation culture: A. cyanogriseus WH1-2216-6 was cultured in seed medium for 5 days, inoculated into 150mL fermentation medium, cultured on a shaking table, fermented for 12 days, and fermented liquid was obtained; among them, the seed medium : 15g peptone, 15g glycerin, 5g soybean powder, 15g soluble starch, 2g calcium carbonate, pH=7.8, 1L aged seawater; fermentation medium: 20g soluble starch, 20g glycerin, 20g peptone, 2g calcium carbonate, XAD-16 macroporous Adsorption resin 50g, aged sea water 1L, pH=7.5.

[0053] Separation and purification: extract the above-mentioned fermentation broth three times with equal volume of ethyl acetate, combine the ethyl acetate extracts and concentrate to obtain a crude extract, add 50mL of 3% HCl solution to each gram of the crude extract, stir, let stand, Extract three times with an equal volume of dichloromethane, adjust the aqueous phase to pH = 8.0 with ammonia water, ...

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Abstract

The invention discloses a 5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound and a preparation method and the application of the 5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound. The 5,5,6-polycyclic tetramic-acid containing macrocyclic lactam compound can be used as a tumor cell proliferation inhibitor or a tumor cell killer or an aspergillus fumigatus growth inhibitor.

Description

technical field [0001] The invention relates to a 5,5,6-polycyclic tetramic acid-containing macrocyclic lactam compound and a preparation method and use thereof. Background technique [0002] "Report on the Status of Nutrition and Chronic Diseases of Chinese Residents (2015)" pointed out that in 2012, the death rate of chronic diseases among residents nationwide was 533 / 100,000, accounting for 86.6% of the total number of deaths. Cardiovascular and cerebrovascular diseases, cancer and chronic respiratory diseases are the main causes of death, accounting for 79.4% of the total deaths, of which the cancer mortality rate is 144.3 / 100,000 (the top five are lung cancer, liver cancer, gastric cancer, esophageal cancer, and colorectal cancer) . According to a report published in Cancer Journal for Clinicians in 2016 (2016,66:115-132), in China, cancer has become the first cause of death among many diseases, and the morbidity and mortality continue to rise. In 2015, China is expect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/08A61K31/407A61P35/00A61P35/02A61P31/10C12P17/18C12R1/04
CPCC07D487/08C12P17/182
Inventor 朱伟明梅显贵王乂刘培培
Owner OCEAN UNIV OF CHINA
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