Indolecarbazole compounds and their preparation methods and applications

A technology for indolecarbazoles and compounds, applied in the field of indolecarbazoles and their preparation, capable of solving problems such as poor specificity

Active Publication Date: 2020-05-22
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, further studies have found that the compound has poor specificity and has a wide range of inhibitory effects on tumor cells and normal cells
[0004] At present, the number of indolecarbazole metabolites derived from microorganisms is quite large, and there are many artificial modifications to them, such as Midostaurin (PKC412), Lestaurtinib (CEP-701), etc., but there is still a large gap for drug development. Therefore, the discovery of good lead compounds is of great significance for preclinical drug development

Method used

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  • Indolecarbazole compounds and their preparation methods and applications
  • Indolecarbazole compounds and their preparation methods and applications
  • Indolecarbazole compounds and their preparation methods and applications

Examples

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Embodiment 1

[0039] 1. Fermentation of compounds

[0040] The marine actinomycete adopts the streptomyces Streptomycessp.CICC 11025 sold by China Common Microorganism Culture Collection and Management Center;

[0041] 1) Inoculate marine actinomycetes in 500mL Erlenmeyer flasks, and each bottle contains 250mL Gaoshi No. 1 liquid medium (each liter contains: 10g of soluble starch; 1g of sodium chloride; 0.5g of dipotassium hydrogen phosphate; heptahydrate and Magnesium sulfate 0.5g; Ferrous chloride 0.01g; Sea salt 25g), the culture condition is 28 ℃, 180rpm in the shaker culture for 3 days, obtain the seed liquid that can be used for fermentation culture;

[0042] 2) Inoculate the seed liquid obtained in step 1) into rice medium (rice medium, made of the following components: 40 g of rice mass; 60 mL of seawater, obtained by high-pressure damp heat sterilization after being placed in a 500 ml Erlenmeyer flask), and inoculated The volume is 12 mL, and it is cultured statically at 28° C. fo...

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Abstract

The invention discloses an indolocarbazole compound. A structural formula of the indolocarbazole compound is shown as a formula I or II. The indolocarbazole compound novel in structural characteristicrespectively has two structural formulas shown as the formulas I and II. The compound is deviated from screen special marine actinomycete and then is obtained through a specific separation and purification mode. The compound has obvious antineoplastic activity and can be used for preparing antineoplastic drugs and protein kinase inhibitors.

Description

technical field [0001] The invention relates to the field of active compound preparation by marine actinomycete culture, in particular to an indolecarbazole compound and its preparation method and application. Background technique [0002] Indolecarbazoles are a class of alkaloids that are widely derived from microbial metabolites. These compounds mainly include staurosporine, K252-a, rebeccamycin, ED-110, azaindolecarbazoles and bisindole Maleimide derivatives. [0003] Studies have found that this type of compound has a wide range of anti-tumor targets, including reported protein kinases, tyrosine kinases, topoisomerases, and enzymes related to tumors and diseases. The most representative indolecarbazole compound, Staurosporine, was discovered in 1986. Studies have reported that it has antifungal, antihypertensive and antitumor effects. It belongs to a class of non-selective protein kinase inhibitors with good cell membrane permeability. The main mechanism of action By i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/23C07H1/06C12P19/26A61P35/00A61P43/00C12R1/465
CPCC07H1/06C07H19/23C12P19/26
Inventor 马忠俊秦乐乐丁婉婧刘美星
Owner 浙江美新控股有限公司
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