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Naphtho thiophene diketone compound and preparation method and application thereof

A technology of naphthothiophenediones and thiophenediones, which is applied in the field of naphthothiophenediones and their preparation, can solve problems such as lack of selectivity, achieve good inhibitory effect, broad application prospects, and significant antitumor activity Effect

Active Publication Date: 2018-05-11
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although multiple ROCK kinase inhibitors have been discovered, only one is on the market, and most lack selectivity

Method used

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  • Naphtho thiophene diketone compound and preparation method and application thereof
  • Naphtho thiophene diketone compound and preparation method and application thereof
  • Naphtho thiophene diketone compound and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0040] 1. Fermentation of compounds

[0041] 1) Inoculate marine Streptomyces CICC 21933 into 500mL Erlenmeyer flasks, each bottle containing 250ml Gaoshi No. 1 liquid medium (based on 1L of medium, 20g of soluble starch, KNO 3 1g;K 2 HPO 4 0.5g, MgSO 4 ·7H 2 O 0.5g, NaCl 0.5g, FeSO 4 ·7H 2(20.01g, surplus is seawater, pH=7.5), at 28 DEG C, 180 rev / min shaker cultures 4 days, obtain the fermentation medium that is inoculated with marine Streptomyces;

[0042] 2) Take 13.5ml of the fermentation medium inoculated with marine Streptomyces in step 1), inoculate it into a solid medium (in 1L, 666g of rice, the remainder of seawater), and culture it statically at 28°C for 30 days to obtain a solid fermentation product.

[0043] 2. Preparation of compounds

[0044] The solid fermentation product was leached three times overnight with an equal volume of ethyl acetate, and the obtained extract was concentrated. The obtained ethyl acetate fraction is subjected to silica gel co...

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Abstract

The invention discloses a naphthothiophene diketone compound with antitumor activity from marine Streptomyces, and a preparation method and application thereof. The structure of the compound is shownin formula I, the compound belongs to a novel structural compound containing sulfur, has significant protein kinase inhibitory activity and anti-tumor activity, can effectively inhibit protein kinasePKC, ROCK2 and the like, can be used for development as a kinase inhibitor; and the compound has a good therapeutic prospect for cancers such as lung cancer, gastric cancer, breast cancer, lymphatic cancer, PDGF dependent tumors and the like. The invention further discloses the preparation method of the compound with antitumor activity, the compound is produced by solid fermentation of marine actinomycetes, through extraction by ethyl acetate or dichloromethane, the culture product is extracted, then through separation and purification by silica gel column chromatography, gel column chromatography and reversed phase chromatography, the compound is obtained, and the method is easy to operate and carry out. The formula I is shown in the description.

Description

technical field [0001] The invention relates to the field of preparing sulfur-containing organic compounds by cultivating marine streptomyces, in particular to a naphthothiophenedione compound with antitumor activity and its preparation method and application. Background technique [0002] There are abundant active secondary metabolites in marine microorganisms, which need to be researched and developed. The study of marine-sourced microorganisms and their secondary metabolites is an important means to solve the current shortage of terrestrial medicinal resources, and is of great significance to the treatment of major human diseases . Most microbial active compounds are produced by microorganisms that are genus-specific rather than taxonomically species-specific. Therefore, even though many marine microorganisms are taxonomically similar to known terrestrial microorganisms, due to adaptation The complex marine environment has produced new specificities, which can often meta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D409/04A61K31/381A61P35/00A61P31/00
CPCC07D409/04
Inventor 马忠俊张大杉丁婉婧
Owner ZHEJIANG UNIV
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