N-13 tyrosine derivative substituted indolocarbazole compound, and preparation method and application of compound

Abstract

The invention discloses an N-13 tyrosine derivative substituted indolocarbazole compound, and a preparation method and application of the compound. The structure of the compound is represented as a formula I; the structural framework of the compound is relatively novel; and the compound has anti-tumor activity and protein kinase inhibiting activity, and can be used for preparing antitumor drugs and protein kinase inhibitors. According to the preparation method of the novel indole carbazole compound, the compound is prepared from a fermentation product of actinomycete Streptomyces sp. CICC 11026 by a rice fermentation method, and can be obtained by performing extraction on the fermentation product by using ethyl acetate and then carrying out separation and purification by gel chromatographyand reversed phase chromatography. The preparation method is easy to operate and implement.

Description

technical field [0001] The invention relates to the field of actinomycete culture and preparation of compounds, in particular to a preparation method of indolecarbazole compounds substituted by N-13 tyrosine derivatives. Background technique [0002] Staurosporine (STA) belongs to the natural product of indolecarbazole alkaloids. A large number of studies have shown that it has strong anti-tumor activity, antibacterial effect, inhibition of platelet aggregation and other pharmacological activities, and has a relatively strong effect on most protein kinases. The strong inhibitory activity is precisely because of its poor selectivity for inhibiting protein kinases, which limits the possibility of its druggability. The subsequently discovered derivatives exhibit selective anti-tumor and protein kinase inhibitory activities, and several have entered clinical trials. At present, its semi-synthetic derivative Midostaurin has made a major breakthrough in the clinical research of t...

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Problems solved by technology

[0002] Staurosporine (STA) belongs to the natural product of indolecarbazole alkaloids. A large number of studies have shown that it has strong anti-tumor activity, antibacterial effect, inhibition of platelet aggregation and other pharmacological activities, and has a relatively strong effect on most protein kinases. Strong inhibitory activity, precisely because of its poor selectivity for inhibiting protein kinases, limits the possibility of its druggability

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