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Application of Puerarin Derivatives in Preparation of Anticancer Drugs and a Drug for Treating Cancer
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A technology of puerarin derivatives and anticancer drugs, applied in the field of medicine
Active Publication Date: 2021-04-09
SHAANXI UNIV OF CHINESE MEDICINE
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However, so far, there is no relevant report about the application of puerarin derivatives in the field of anticancer in this field
Method used
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preparation example Construction
[0027] The present invention has no special requirements for the preparation method of puerarin derivatives, and can be prepared by methods well known to those skilled in the art; in specific embodiments of the present invention, the puerarin derivatives are preferably prepared by the following steps:
[0028] (1) Puerarin derivatives, potassium carbonate, compound A and DMF are mixed and reacted to obtain R 1 Substituted puerarin derivatives; the compound A is a halogenated hydrocarbon, a substituted benzyl bromide or a halogenated ether; the halogenated hydrocarbon includes a halogenated alkane or a halogenated aromatic hydrocarbon;
[0029] (2) the R 1 Substituted puerarin derivatives, potassium carbonate, compound B and DMF were mixed and reacted to obtain R 1 and R 2 Substituted puerarin derivatives; the compound B is methyl iodide, substituted methyl iodide, diethyl sulfate, ethyl iodide, substituted ethyl iodide or halogenated ether.
[0030] In the present invention...
Embodiment 1～7
[0043] Other conditions are the same as in Comparative Example 1, only n-butane bromide is replaced by octane bromide, p-chlorobenzyl bromide, p-methoxybenzyl bromide, pentane bromide, hexane bromide, and p-methylbenzyl bromide , chloromethyl ether, and the obtained products are respectively recorded as compounds 1b~1h, and the specific structures are shown in Table 1.
Embodiment 8
[0045] Compound 1a (0.2mmol) and K 2 CO 3 (0.24mmol) was added to 5mL DMF, stirred under ice bath, slowly added iodomethane (0.24mmol), after the dropwise addition, the reaction mixture was dissolved in CaCl 2 Under the protection of a drying tube, the reaction was carried out at room temperature for 5 h.
[0046] The reaction mixture was slowly poured into 20 mL of water, and the aqueous phase was washed with CH 2 Cl 2 Extraction (20mL×3). The organic phases were combined, washed with saturated brine, anhydrous Na 2 SO 4 Dry, evaporate the solvent on a rotary evaporator, and purify by silica gel column chromatography to obtain R 1 and R 2 The substituted puerarin derivative is denoted as compound 2a, and its specific structure is shown in Table 1.
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Abstract
The invention relates to the technical field of medicine, and provides an application of a puerarin derivative in the preparation of an anticancer drug and a drug for treating cancer. The present invention has found that puerarin derivatives have obvious inhibitory activity on various tumor cells such as A549, Bel-7404, HCT-116, etc., and their application in the preparation of anticancer drugs has broad application prospects and is expected to become a clinically effective drug. new anticancer drugs.
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to the application of puerarin derivatives in the preparation of anticancer drugs and a drug for treating cancer. Background technique [0002] Puerarin is a flavonoid glycoside extracted from the root of Pueraria mirifica, a leguminous plant. It is an isoflavone derivative with a crown-expanding effect isolated from Pueraria lobata, a traditional Chinese medicine. It has antipyretic, sedative and increased coronary blood flow It has a protective effect on acute myocardial hemorrhage caused by vasopressin, and is clinically used for coronary heart disease, angina pectoris, and hypertension. [0003] Puerarin chemical name: 4',7-dihydroxy-8-β-D-glucosyl isoflavone, the structural formula is as follows [0004] [0005] In recent years, in order to improve the pharmacological activity of puerarin, researchers have used the chemical activity of the phenolic hydroxyl group at the 7...
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