Chrysin non-natural amino acid derivative as well as preparation method and application thereof

An unnatural amino acid, chrysin technology, applied in the field of medicine, can solve the problems of poor water solubility, less intestinal absorption, easy metabolic inactivation and so on
CN108101892AActive Publication Date: 2018-06-01SHIJIAZHUANG UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHIJIAZHUANG UNIVERSITY
Publication Date
2018-06-01

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Abstract

The invention discloses a chrysin non-natural amino acid derivative or pharmacologically-acceptable hydrate and salt thereof. The chrysin non-natural amino acid derivative comprises a stereoisomer ora tautomer. The chrysin non-natural amino acid derivative comprises the following preparation steps: preparing 5-hydroxy-7-propargylflavone by chrysin and propargyl bromide under the action of alkali;preparing (L / D)-N3-Boc amino acid methyl ester by (L / D)-halogenated-Boc amino acid methyl ester and NaN3 under the action of CuI / L-proline sodium; reacting the 5-hydroxy-7-propargylflavone and the (L / D)-N3-Boc amino acid methyl ester under the action of CuSO4.5H2O / sodium ascorbate, removing Boc groups and hydrolyzing to prepare the chrysin amino acid derivative. The chrysin non-natural amino acidderivative disclosed by the invention has an anti-cancer effect and can be used in preparation of an anti-cancer drug.
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Description

technical field

[0001] The invention relates to unnatural amino acid derivatives of chrysin and their application in pharmacy, belonging to the technical field of medicine. Background technique

[0002] Chrysin (5,7-dihydroxyflavone) is a flavonoid compound that widely exists in nature and has a wide range of pharmacological activities such as antibacterial, antioxidant, antitumor, anti-inflammatory, antidiabetic, and anxiolytic. Recent studies have shown that it can also prevent cisplatin-induced organ toxicity and improve cognitive deficits and brain damage caused by intermittent hypoxia. However, due to its poor water solubility and low intestinal absorption, it is easily metabolized and inactivated in the body. In order to improve its pharmacological activity, its structural modification and transformation are of great significance for obtaining new drug candidates with high efficiency and low toxicity.

[0003] Amino acid is the basic unit of protein, and as an import...

Claims

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