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Tripterygium wilfordii diterpenes diterpenoids lactones derivative and uses thereof

A technology of triptolide and tripterygium, applied in the field of tripterygium diterpenoid lactone derivatives and its application, achieving good research and application value, and obvious dose-dependent effects

Inactive Publication Date: 2008-09-03
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term research results at home and abroad show that the toxic and side effects of diterpenoid lactone compounds of tripterygium wilfordii are mainly reflected in the reproductive system, but the previous research on the antitumor efficacy of this type of compound has never been systematically administered to reproductive system tumors. efficacy evaluation

Method used

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  • Tripterygium wilfordii diterpenes diterpenoids lactones derivative and uses thereof
  • Tripterygium wilfordii diterpenes diterpenoids lactones derivative and uses thereof
  • Tripterygium wilfordii diterpenes diterpenoids lactones derivative and uses thereof

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Embodiment Construction

[0017] A preferred embodiment of the present invention is C in general formula (1) 14 XY is (14S)-14,21-epoxy structure, W and Z are respectively connected in C 12 and C 13 Oxygen in the α (S) configuration of the position, P is hydrogen or hydroxyl in the α (R) configuration, and Q is a hydrogen diterpene lactone derivative of Tripterygium wilfordii, namely the compound shown in the following general formula (2):

[0018]

[0019] Another preferred embodiment of the present invention is C in general formula (1) 14 XY is (14S)-14,21-epoxy structure, W is halogen in β(R) configuration, Z is hydroxyl in α(R) configuration, P is hydrogen or hydroxyl in α(R) configuration, Q Be the tripterygium wilfordii diterpenoid lactone derivative of hydrogen, namely the compound shown in the following general formula (3):

[0020]

[0021] Another preferred embodiment of the present invention is C in general formula (1) 14 XY is (14S)-14,21-epoxy structure, W and Z are respectively ...

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Abstract

The invention relates to tripterygium wilfordii diterpenes lactone derivates represented by the formula (1), optical isomers thereof and pharmaceutically acceptable salts and hydrate thereof, wherein C5 and C6 are combined by C-C or C=C bind; P and Q represent hydrogen, oxygen, hydroxyl, halogen, sulfhydryl, C1-C6 alkoxyl, C1-C6 alkylamino radical, or C1-C6 alksulfhydryl combined on positions C5 or C6 respectively when C5 and C6 are combined by C-C bind; and C14XY is combined at the position C14 with the structure shown in the view, and W and Z represent oxygen, hydroxyl, halogen, sulfhydryl, C1-C6 alkoxyl, C1-C6 alkylamino radical, or C1-C6 alksulfhydryl combined on positions C12 or C13 respectively, '-'combined with X, Y, Z, W, P and Q represent '' '' or '' ''. The invention further relates to a synthetic method thereof and the applications on preparing the medicine for treating hypertrophic tumor.

Description

technical field [0001] The invention relates to tripterygium wilfordii diterpene lactone derivatives and their application in the preparation of medicines for treating proliferative tumor diseases. Background technique [0002] Tripterygium wilfordii Hook F (Tripterygium wilfordii Hook F), also known as Huangteng, belongs to the genus Tripterygium wilfordii Hook F. There are four kinds in China, three of which are used as medicine. They are mainly produced in the middle and lower reaches of the Yangtze River, and are mainly produced in the Yangtze River Basin. And the Kunming Mountain Begonia in the southwest and the Northeast Tripterygium vine, which is mainly produced in the Northeast and Japan. Tripterygium wilfordii was first recorded in "Shenlong Materia Medica", and its main chemical components include diterpenes, triterpenes, sesquiterpenes, alkaloids, etc. Studies in the past two decades have shown that it has anti-tumor, anti-inflammatory, immunosuppressive, and ant...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00C07J71/00A61K31/585A61P35/00
CPCA61P35/00C07J21/00C07J33/00C07J71/00C07J73/003
Inventor 李援朝李征周兆丽林莉萍缪泽宏任进李川甘勇丁健冯慧瑾
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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