Staurosporine derivatives, preparation method and application thereof

A technology for staurosporine and derivatives, applied in the field of staurosporine derivatives and their preparation, can solve problems such as poor selectivity, and achieve the effects of simple experimental operation, good application prospects, and easy production expansion

Active Publication Date: 2019-11-26
浙江美新控股有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, these compounds are usually poorly selective and have inhibitory effects on both cancer cells and normal cells

Method used

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  • Staurosporine derivatives, preparation method and application thereof
  • Staurosporine derivatives, preparation method and application thereof
  • Staurosporine derivatives, preparation method and application thereof

Examples

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Embodiment Construction

[0035] Below in conjunction with specific embodiment, further illustrate the present invention. It should be understood that these examples are only used to illustrate the present invention and are not intended to limit the scope of the present invention. The operating methods not indicated in the following examples are generally in accordance with conventional conditions, or in accordance with the conditions suggested by the manufacturer.

[0036] In this example, the staurosporine compounds of the above structural formulas 1-14 were obtained by the following method.

[0037] Actinomycetes Fermentation

[0038] The actinomycete adopts the streptomyces Streptomycessp.CICC 11031 sold by China Common Microorganism Culture Collection and Management Center;

[0039] 1) Inoculate the actinomycetes in Gao's No. 1 medium, culture at 28°C, and culture on a shaker at 180rpm for 4 to 6 days to obtain seed liquid;

[0040] Gaoshi No. 1 medium: soluble starch 20g, KNO 3 1g, K 2 HPO ...

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Abstract

The invention discloses staurosporine derivatives, which can be used for development of anti-tumor related drugs and drugs for protein kinase, tyrosine kinase and other kinase inhibition related diseases. The invention also provides a preparation method of the staurosporine derivatives. The method includes: subjecting actinomycetes to fermentation in a rice solid medium, then performing ethyl acetate extraction to obtain a fermentation crude extract, and employing gel column choromatography, silica gel column chromatography, medium pressure liquid chromatography and high performance liquid chromatography for separation and purification, thus obtaining the product. The method is easy to operate and implement. The staurosporine derivatives provided by the invention have novel structure types, and are firstly discovered in natural products. The staurosporine derivatives are simple in experimental operation, are easy for expanded production, and have good application prospects.

Description

technical field [0001] The invention relates to the field of preparing active compounds from actinomycete fermentation products, in particular to a class of staurosporine derivatives and a preparation method and application thereof. Background technique [0002] Malignant tumors are diseases that seriously threaten human health. With the gradual aging of my country's population, the acceleration of industrialization and urbanization, and the accumulation of risk factors such as unhealthy lifestyles and the environment, the prevention and control of malignant tumors is extremely severe. [0003] According to the cancer statistics released by the National Cancer Center in January 2019, the death of malignant tumors accounted for 23.91% of all the deaths of residents, and the incidence and death of malignant tumors have continued to rise in the past ten years. Lung cancer, liver cancer, upper digestive system tumors and colorectal cancer, male prostate cancer, and female breast...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/14C07D498/22C07H1/00C07H17/02C07D491/22A61P35/00A61P35/02A61P31/18A61P25/28C12P17/18C12P19/60C12R1/465
CPCA61P25/28A61P31/18A61P35/00A61P35/02C07D487/14C07D491/22C07D498/22C07H1/06C07H9/06C07H19/23C12P17/182C12P17/188C12P19/26
Inventor 马忠俊王金慧丁婉婧李嘉琦张浩健刘美星
Owner 浙江美新控股有限公司
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