Compounds with anti-tumor activity as well as preparation method and application of compounds

Abstract

The invention discloses compounds with anti-tumor activity as well as a preparation method and an application of the compounds. The structures of the compounds are shown as formulae (I) and (II) in the description. The compounds can be used for preparing drugs for treating diseases such as acute leukemia and chronic leukemia associated with protein kinase inhibition, lymphoma, breast cancer, lung cancer and other cancer, acquired immune deficiency syndrome, coronary heart disease, diabetes mellitus, senile dementia and the like. The invention further provides the preparation method of the compounds with the anti-tumor activity. According to the preparation method, marine actinomycete is fermented with a rice solid medium, a fermentation product obtained after extraction with ethyl acetate is subjected to separation and purification with gel column chromatography and preparative liquid chromatography, and the method is easy to operate and implement.

Description

technical field [0001] The invention relates to the field of preparing active compounds by cultivating marine actinomycetes, in particular to a compound with antitumor activity and its preparation method and application. Background technique [0002] Since the indolecarbazole alkaloid staurosporine (STA) was isolated from Streptomyces clavicularis (ATCC55006) in 1977, it has attracted attention due to its wide range of pharmacological activities, such as: anti-tumor, anti-bacterial, anti-hypertensive, And it has a strong inhibitory effect on protein kinase C (PKC), tyrosine kinase, topoisomerase, extracellular regulatory protein kinase, etc., especially the inhibitory activity on protein kinase C (PKC) (IC 50 =2.7nM), but later studies found that STA had poor specific selectivity to normal cells and tumor cells, and could not be used as a drug, so the discovery and application of its derivatives continued to deepen. PKC is a group of phospholipid-dependent Ca 2+ Activated ...

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Problems solved by technology

[0002] Since the indolecarbazole alkaloid staurosporine (STA) was isolated from Streptomyces clavicularis (ATCC55006) in 1977, it has attracted attention due to its wide range of pharmacological activities, such as: anti-tumor, anti-bacterial, anti-hypertensive, And it has a strong inhibitory effect on protein kinase C (PKC), tyrosine kinase, topoisomerase, extracellular regulatory protein kinase, etc., especially the inhibitory activity on protein kinase C (PKC) (IC 50 =2.7nM), but later studies found that STA had poor specific selectivity to normal cells and tumor cells, and could not be used as a drug, so the discovery and application of its derivatives continued to deepen

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