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Application of o-quinone structure-contained compounds in preparing tumor resistant medicament

An anti-tumor drug and compound technology, applied in the application field of preparing anti-tumor drugs, can solve the problems of unsatisfactory antibacterial and anti-tumor activity, low content and the like

Inactive Publication Date: 2011-07-20
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The content of Mansonone F in nature is very low, it is difficult to obtain in large quantities, and its antibacterial and anti-tumor activity is not ideal, so we use Mansonone F as the lead compound, modify its structure, and study other possible pharmacological effects to seek anti-tumor The new drug of Mansonone F derivatives with better activity and better anti-drug resistance is of great significance for the treatment of anti-tumor and drug-resistant tumors

Method used

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  • Application of o-quinone structure-contained compounds in preparing tumor resistant medicament
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  • Application of o-quinone structure-contained compounds in preparing tumor resistant medicament

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Embodiment Construction

[0020] 1. Preparation of the series of compounds involved in the present invention.

[0021] The preparation method of the compound represented by general formula (I) involved in the present invention can be carried out with full reference to existing patents 200410077779.3, 200410077778.9 and WO 01 / 51004A2. According to the patent, we have synthesized compounds III-J1~6, V-J1~ 3. V-J6, VII-J1, VIII-J1, IV-J2~6, VI-J2, VI-J3, VI-J6 compounds, the compound spectrum data obtained are the same as the above patent results, and will not be listed here out.

[0022] Compound structures and corresponding numbers are as follows:

[0023]

[0024] VIII-J1: R1=Cl, R2=CH3, R3=OCOPh VII-J1: R1=H, R2=CH3, R3=H

[0025]

[0026] D-1 D-2 D-3 D-4 D-5

[0027] 2. Cytotoxic activity test experiment

[0028] Cytotoxic activity of the synthesized compounds III-J1~6, V-J1~3, V-J6, VII-J1, VIII-J1, IV-J2~6, VI-J2, VI-J3, VI-J6 Test, with 10-hydroxycamptothecin, mansononeF, etoposide an...

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Abstract

The invention discloses application of a series of non-6-site methyl substituted o-quinone structure-contained compounds in aspect of preparing anticancer medicaments. The compounds are derivatives obtained by reforming a Mansonone F (mansonone, Msn) structure, and the compounds comprise the structural formula shown in the specification, wherein A expresses the formula shown in the specification. The anticancer cell toxic activity IC50 of the o-quinone structure-contained compounds disclosed by the invention is equal to 1-20mu M(NCI-460 and PC-3 cell strain). The activity of certain compounds is tens of times stronger than that of etoposid and is 50 times stronger than that of a natural product Mansonone F. The invention has favorable application prospect.

Description

field of invention [0001] The invention relates to an antitumor compound, in particular to the application of a derivative of Mansonone (Msn) F containing an o-quinone structure in the preparation of antitumor drugs. Background technique [0002] [0003] Mansonone compounds are compounds with a quinone structure in a class of natural products. They are mainly extracted and isolated from the heartwood of mansonia altissima and ulmus glabra. They are used as phytoalexins. It is a class of substances that plants themselves produce and gradually accumulate to fight against foreign bacterial or fungal infections. It can be used in the treatment of the Dutch elm disease (DED) fungus, a plant disease that once caused the death of large elm trees in Europe and North America. This type of compound has a novel structure, and some compounds have the structure of oxabenzobenzopyran (oxaphenalene), which is relatively rare in natural products. According to research, this type of co...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P35/00
Inventor 黄世亮古练权黄志纾区杰彬黄志鸿
Owner SUN YAT SEN UNIV
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