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Compound with protein kinase inhibiting activity as well as preparation method and application of compound

A technology for protein kinase inhibitory compounds, which is applied in the field of compounds with protein kinase inhibitory activity and their preparation, can solve the problems of poor selectivity and inability to make medicines, and achieve the effect of being conducive to large-scale industrial production and broad application prospects

Active Publication Date: 2017-06-13
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have shown that STA is a strong PKC (protein kinase C) inhibitor (IC 50 =2.7nM), however, it cannot be drugged due to poor selectivity

Method used

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  • Compound with protein kinase inhibiting activity as well as preparation method and application of compound
  • Compound with protein kinase inhibiting activity as well as preparation method and application of compound
  • Compound with protein kinase inhibiting activity as well as preparation method and application of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] 1. Fermentation of compounds

[0055] The actinomycete adopts the streptomyces Streptomycessp.CICC 10513 sold by China Industrial Microorganism Culture Collection Management Center;

[0056] 1) inoculate actinomycetes in 500mL Erlenmeyer flasks, each bottle contains 250mL of Gaoshi No. 1 medium, culture on a shaker at 28°C and 180rpm for 3 days, and obtain seed liquid inoculated with actinomycetes;

[0057] 2) Inoculate the actinomycetes inoculated in step 1) into rice medium (rice medium, made of the following components: rice 40g; seawater 60mL), the inoculation volume is 10mL, and cultured statically at 28°C for 30 In 1 day, a solid fermentation product containing the compound having protein kinase inhibitory activity of the present invention was obtained.

[0058] 2. Preparation of compounds

[0059] The solid fermented product containing the compound having protein kinase inhibitory activity of the present invention is extracted three times with ethyl acetate, an...

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Abstract

The invention discloses a compound with protein kinase inhibiting activity as well as a preparation method and application of the compound. The compound has a structure shown as a formula I, a formula II and a formula III. The compound provided by the invention can be used for medicines for treating cancers related with kinase inhibition, such as acute and chronic leukemia, lymphoma, breast cancer, lung cancer and sarcoma, and diseases including acquired immunodeficiency syndrome and Alzheimer's disease and the like. The invention further discloses the preparation method of the compound with the protein kinase inhibiting activity; the compound is produced through solid fermentation on rice by utilizing actinomyces; a fermented product is extracted through ethyl acetate and then is subjected to silica-gel column chromatography, gel column chromatography and reversed-phase chromatography separation and purification to obtain a product; the preparation method is easy to operate and implement. (The formula I, the formula II and the formula III are shown in the description.).

Description

technical field [0001] The invention relates to the field of bacterial culture and preparation of compounds, in particular to a compound with protein kinase inhibitory activity and its preparation method and application. Background technique [0002] Indolecarbazoles are a class of alkaloids isolated from microbial fermentation broths. They have significant antitumor activity and mainly act on various kinases, topoisomerases and cell cycle regulatory factors in cell signal transduction pathways. Staurosporine (STA) is an indolecarbazole alkaloid isolated from Streptomyces staurosporeus. Studies have shown that STA is a strong PKC (protein kinase C) inhibitor (IC 50 =2.7nM), however, it cannot be drugged due to poor selectivity. A number of staurosporine derivatives are currently under clinical research as antineoplastic drugs. Naturally derived staurosporine derivative UCN-01 is currently in phase II clinical research for the treatment of breast cancer and lymphoma. The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H9/06C07H19/23C07H1/00C12P19/38A61P35/00A61P35/02A61P31/18A61P25/28C12R1/04
CPCC07H1/00C07H9/06C07H19/23C12P19/38
Inventor 马忠俊胡志娟陈喆刘美星徐成栋
Owner 浙江美新控股有限公司
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