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Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine

A kind of staphylophyllin and synthetic method technology, applied in the direction of anti-tumor drugs, drug combination, organic chemistry, etc., can solve the problems of low lipophilicity, low bioavailability of 5-fluorouracil, affecting anti-tumor efficacy, etc., and achieve good anti-tumor The effect of action

Inactive Publication Date: 2011-06-15
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to significant first-pass metabolism and low lipophilicity, the bioavailability of 5-fluorouracil is low, which affects the anti-tumor efficacy, and its therapeutic dose is close to the toxic dose

Method used

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  • Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine
  • Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine
  • Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine

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Embodiment 1

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Abstract

The invention relates to a ampelopsin derivative, wherein R1-R5 are represented as formula II or H, and R1-R5 are not all as H. The invention further relates to the synthesis method of the derivative and relative application for preparing anti-cancer drug.

Description

technical field The present invention relates to a compound, its synthesis method and its application in the preparation of anti-tumor drugs, in particular, it relates to a staphylophyllin derivative, its synthesis method and its application in the preparation of anti-tumor drugs. Background technique Ampeloptin, also known as dihydromyricetin, chemically named "3,5,7,3',4',5'-hexahydroxy-dihydroflavone", is a plant of the genus Ampeloptin The main component of Ampelopsis cantoniensis (Hook.et Am.) Planch.], or Ampelopsis grossedentata (Hand.-Mazz.) W.T.Wang], belongs to dihydroflavonols. In recent years, it has been found that staphylophyllin is a strong tyrosinase inhibitor [Liu Deyu, Lei Huanqiang. Inhibition of myricetin and staphylophyllin on tyrosinase. Journal of Biochemistry, 1996, 12( 5): 618-620]. Staphylococcus can significantly inhibit the proliferation of human promyelocytic leukemia HL-60 and K562 cells, human nasopharyngeal carcinoma HK-1 cells, human liver ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/12A61K31/506A61P35/00
Inventor 刘德育
Owner SUN YAT SEN UNIV