Staurosporine derivative and preparation method and application thereof
A technology for staurosporine and derivatives, applied in the field of staurosporine derivatives and their preparation, which can solve the problems of poor selectivity and achieve the effects of simple experimental operation, good application prospects, and easy expansion of production
Active Publication Date: 2020-06-19
浙江美新控股有限公司
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Problems solved by technology
[0008] However, these compounds are usually poorly selective and have inhibitory effects on both cancer cells and normal cells
Method used
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[0036] 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.
[0037] In this example, the staurosporine compounds of the above structural formulas 1-14 were obtained by the following method.
[0038] Actinomycetes Fermentation
[0039] The actinomycete adopts the streptomyces Streptomycessp.CICC 11031 sold by China Common Microorganism Culture Collection and Management Center;
[0040] 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;
[0041] Gaoshi No. 1 medium: soluble starch 20g, KNO 3 1g, K 2 HPO ...
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Abstract
The invention discloses a staurosporine derivative which can be used for developing anti-tumor related drugs and drugs for inhibiting diseases related to protein kinase, tyrosine kinase and other kinases. The invention also provides a preparation method of the staurosporine derivative, the staurosporine derivative is prepared by fermenting actinomycete rice solid culture medium and extracting by ethyl acetate to obtain a fermented crude extract, and the fermented crude extract is separated and purified by gel column chromatography, silica gel column chromatography, medium-pressure preparativechromatography and high performance liquid chromatography, and is easy to operate and implement. The staurosporine derivative disclosed by the invention is relatively novel in structural type, and isfound in natural products for the first time; the method is simple in experimental operation and easy to expand production, and has a good application prospect.
Description
[0001] This application is a divisional application of "a class of staurosporine derivatives and their preparation methods and applications". The filing date of the original application is September 19, 2019, and the application number of the original application is 201910887005.3. technical field [0002] 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 [0003] 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. [0004] According to the cancer statistics released by the National Cancer Center in January 2019, the death of...
Claims
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IPC IPC(8): C07D487/14C07D498/22C07H1/00C07H19/23C07H9/06C07D491/22A61P35/00A61P35/02A61P31/18A61P25/28C12P17/18C12P19/26C12R1/465
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