- 5-substituted icaritin derivative and anti-tumor application thereof
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The invention provides a 5-substituted icaritin derivative as shown in a structural formula 4, and a preparation method and anti-tumor application thereof. Activity tests prove that the 5-substitutedicaritin derivative as shown in 4 is designed and synthesized in the invention, is a suitable anti-tumor candidate drug, and especially can be used as an anti-liver cancer candidate drug, an anti-colon cancer candidate drug, an anti-lung cancer candidate drug and an anti-colon cancer candidate drug. Besides, the preparation method of the 5-substituted icaritin derivative is high in synthetic routeyield and easy to operate and implement.
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Paragraph 0016-0018
(2020/11/26)
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- Selective alkylation of β-anhydroicaritine and their biological evaluation on anticancer
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A convenient and selective alkylation of icaritin has been developed. The methodology involved initial formation of β-anhydroicaritine (3) under acidic conditions followed by selective methylation at the C-3 position and then alkylation at C-5 position. Several alkylated β-anhydroicaritine derivatives were synthesised using this methodology. These newly synthesised derivatives, especially the compounds 5b, 5c and 5j, significantly suppressed cell proliferation when tested against cancer cell lines in?vitro. Compound 5j (R = Bn) exhibited a competitive inhibition against MCF7 in?vivo compared to tamoxifen.
- Cui, Hanqi,Pu, Yue,Wang, Xianheng,Wang, Yuhe,Zhao, Changkuo
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supporting information
(2020/11/19)
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- Flavone derivative and preparation method and medical application of flavone derivative
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The invention relates to a flavone derivative and a preparation method and medical application of the flavone derivative. The flavone derivative is prepared through a mode that anhydroicaritin is taken as a mother nucleus, and group addition and reduction are conducted. It is proved through a pharmacological experiment that the flavone derivative has the pharmacological effect of activating endogenous stem cells in the body, achieves the effects of repairing injury-type pathological changes of blood vessel cells, nerve cells, endothelial cells and the matrix and recovering functions, can be used for preparing medicines for repairing the tissue-injury pathological changes and has a good prospect in preparing medicines for conducting rehabilitation treatment on erectile dysfunction pathological changes.
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- Preparation and medical application methods of icaritin derivative
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The invention relates to preparation and medical application methods of an icaritin derivative. The preparation method comprises taking trihydroxyacetophenone, chloromethyl methyl ether and the like as initial raw materials to connect isopentene groups to an 8th carbon through vicinal rearrangement, then performing serial reaction of formation of a flavone framework, and lastly, performing dehydration to introduce propylene groups to synthesize the icaritin derivative. The preparation method of the icaritin derivative is low in the cost of the synthetic routes, simple in operation, high in recovery rate and applicable to industrial production. Pharmacological effect experiments prove that the icaritin derivative has the pharmacological effect of activating organism endogenous stem cells and achieves the rehabilitation function of repair traumatic pathological changes of blood vessels, nerves, endothelial cells and matrixes and can be applied to preparing drugs for repairing traumatic pathological changes of tissues, thereby having a good prospect in fields such as drugs for rehabilitation of pathological changes of erectile dysfunction.
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- Method for preparing dewatered icaritin through total-synthesis
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The invention provides a method for preparing dewatered icaritin through total-synthesis. The method includes the steps of connecting an isopentene group to 8th-position carbon through ortho-positionrearrangement with methoxybenzoyl chloride, isoprenyl bromide and the like as the raw materials by means of trihydroxyacetophenone, and conducting the forming series reaction of a flavone framework toobtain the dewatered icaritin. The defects that in a traditional method of introducing an isopentene group, the yield is low, catalysts are expensive and lots of byproducts are produced are overcome,and the method is low in cost, simple in operation, good in yield and suitable for industrial production.
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- Synthesis and antimultidrug resistance evaluation of icariin and its derivatives
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A series of icariin derivatives were synthesized. Their multidrug resistance (MDR) reversal activities were evaluated by MTT assay and the results indicated that the derivatives were the potent modulators of MDR. It was showed that the derivatives signifi
- Liu, Dong-Fang,Li, Yan-Ping,Ou, Tian-Miao,Huang, Shi-Liang,Gu, Lian-Quan,Huang, Min,Huang, Zhi-Shu
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supporting information; experimental part
p. 4237 - 4240
(2010/04/26)
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- TWO FLAVONOL GLYCOSIDES FROM THE UNDERGROUND PARTS OF VANCOUVERIA HEXANDRA
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Two new flavonol glycosides were isolated from the roots and rhizomes of Vancouveria hexandra.The glycosides were determined by chemical and spectral means to be anhydroicaritin 3-galactosyl(1->3)rhamnoside-7-glucoside and hydroicaritin 3-3)rhamnoside>-7-glucoside.
- Mizuno, Mizuo,Iinuma, Munekazu,Tanaka, Toshiyuki,Sakakibara, Norio,Murata, Jin,et al.
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p. 1277 - 1281
(2007/10/02)
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