Baicalein derivative and preparation method thereof

A technology for baicalein and derivatives, which is applied in the field of medicine, can solve the problems of poor water solubility, low bioavailability, limited application and the like of baicalein, and achieves the effects of low cost, simple reaction operation and easy handling.

Inactive Publication Date: 2017-01-18
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, baicalein has disadvantages such as poor water solubility and low bioavailability, which limit its application in drug therapy to...

Method used

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  • Baicalein derivative and preparation method thereof
  • Baicalein derivative and preparation method thereof
  • Baicalein derivative and preparation method thereof

Examples

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preparation example Construction

[0042] Preparation of (Compound IVb)

[0043] The preparation of compound IVb is similar to the preparation of compound IVa, substituting 1-azido-4-methylbenzene with 1-azido-2-methoxybenzene; 1 H NMR (400 MHz, DMSO- d 6 ) δ 12.57 (s, 1H), 7.93 – 7.89 (m, 2H), 7.59 – 7.49 (m, 3H), 7.46 – 7.40 (m, 1H), 7.40 – 7.31 (m, 3H), 6.93 (s, 1H) ), 6.69 (s, 1H), 5.61 – 5.41 (m, 3H), 2.22 (s, 3H); 13 C NMR (101 MHz, DMSO- d 6 ) δ 182.38,163.32,153.21,149.61,146.46,142.21,136.18,133.04,132.02,131.43,130.86,130.38,129.92,129.17,127.06,126.65,126.36,126.03,105.60,104.76,92.69,62.31,17.44; HRMS ( m / z): calcd for C 25 H 20 N 3 O 5 [M+H] + : 442.1397, found: 442.1397.

[0044] Example 5: 5,6-Dihydroxy-2-phenyl-7-((1-( m -tolyl)-1 H -1,2,3-triazol-4-yl)methoxy)-4 H -chromen-4-one (FZU-0016-021)

[0045] Preparation of (Compound IVc)

[0046] Compound IVc was prepared analogously to compound IVa, substituting 1-azido-4-methylbenzene for 1-azido-3-methoxybenzene. 1 H NMR (400...

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Abstract

The invention discloses a baicalein derivative and a preparation method and application thereof. The general formula I of the baicalein derivative is as shown in the specification. In the formula, R1 is hydrogen, propargyl group, 2-propylamyl ester or methylenetriazole; and R2 is propargyl group or methylenetriazole. The compound can remarkably inhibit proliferation and survival of various hematological tumor cells such as leukemia cells and inhibit tumor cell signaling pathway at multiple targets so as to induce tumor cell apoptosis and achieve the effect of treating tumor diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a class of baicalein derivatives and a preparation method thereof. Background technique [0002] Flavonoids are widely distributed in vegetables, fruits and herbal medicinal materials, and have extremely high medicinal value, such as antioxidant, anti-inflammatory, anti-tumor, and immunomodulatory functions, and their development is of great significance. Chinese medicine Scutellaria (Scutellaria baicalensis) Scutellaria baicalensis Georgi ) was first recorded in "Shen Nong's Materia Medica", bitter in taste, cold in nature, functions to relieve real fire, dehumidification and heat, antibacterial, heat removal, detoxification, sedation, blood pressure, gallbladder and other effects. Baicalin and baicalin (baicalein) are the main flavonoids contained in Scutellaria baicalensis, and both have the same flavonoid parent structure. Baicalin and baicalein have various ...

Claims

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Application Information

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IPC IPC(8): C07D405/14C07D405/12C07D311/30A61K31/352A61K31/4192A61P35/00A61P35/02
CPCC07D405/14C07D311/30C07D405/12
Inventor 陈海军胡建达陈英玉吴建磊刘炫萍李财龙
Owner FUZHOU UNIV
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