Antitumor application of phenolic nitrogen oxides as sirtuin inhibitors

A sirtuin, nitrogen oxide technology, applied in the field of disease

Active Publication Date: 2019-08-23
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] With the deepening of molecular biology research, the anti-tumor mechanism of HDAC inhibitors has been gradually revealed, but there is still a question of whether HDACs have an effect on other molecular targets, HDAC inhibitors that are selective for HDACs subtypes, and improve HDAC inhibition In vivo stability of the drug, etc.

Method used

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  • Antitumor application of phenolic nitrogen oxides as sirtuin inhibitors
  • Antitumor application of phenolic nitrogen oxides as sirtuin inhibitors
  • Antitumor application of phenolic nitrogen oxides as sirtuin inhibitors

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Embodiment Construction

[0030] The technical solution of the present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments.

[0031] 1. Synthesis of Compound Y-1:

[0032]

[0033] Take a 100mL eggplant-shaped bottle and dry it, weigh p-hydroxybenzoic acid (1160mg, 8.40mmol), add tetrahydrofuran (THF, 10mL) to dissolve, stir, add aniline (PhNH 2 , 1mL) and thionyl chloride (SOCl 2 ,0.874mL) after 0.5h, put it at room temperature to react for 26h, the reaction was completed, concentrated, and the silica gel column was eluted with dichloromethane:methanol=60:1,50:1,40:1 gradient to obtain white powder Y-1 312mg , the yield is 26.9% 1 H-NMR (400MHz, DMSO) δ (ppm): 7.80-7.77 (m, 2H) 7.61-7.59 (d, 2H, J = 8Hz) 7.37-7.33 (m, 2H) 7.14-7.11 (d, 1H) 6.91 -6.89(d,2H,J=8Hz); 13 C-NMR (300Hz, DMSO) δ (ppm): 165.03, 160.49, 139.43, 128.41, 125.35, 123.14, 120.20, 114.81.

[0034] 2. Synthesis of Compound Y-2:

[0035]

[0036] Take Y-1 (300mg...

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Abstract

The invention discloses anti-tumor application of tocopheroxyl nitrogen oxide as an HDAC (Histone Deacetylase) inhibitor. A compound has a structural general formula as shown in a formula (I), and the compound has a potential inhibition effect on HDAC, so that more nitrogen and oxygen can be further provided for a ZBG (Zinc Binding Group), multi-length survey and the like can be carried out on a linker, structure modification can be carried out on the existing basis, and the functions of an inhibitor having good selectivity on HDAC subtype and other target points are expected to be found. According to the anti-tumor application disclosed by the invention, synthetic raw materials are relatively cheap, the technology is simple, the purity is higher, the cost is lower, and used reagents are all relatively safe. The compound is expected to be used as a novel HDAC inhibitor type anti-tumor medicine which is strong in selectivity, high in efficiency and low in toxicity.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to the preparation, use and derivatives of phenolic nitrogen oxides as novel histone deacetylase inhibitors, the pharmaceutical composition containing the compound, and the preparation method of the compound And the anti-tumor application of the compound, relates to the application of the compound in diseases, such as anti-tumor cells. Background technique [0002] HDAC inhibitors have been clinically used in the treatment of tumor diseases, and have shown good prospects for clinical application. HDAC inhibitors can have multiple effects on the physiological functions of tumor cells, such as inhibiting tumor cell proliferation, inducing cell cycle arrest, inducing tumor cell apoptosis, and inhibiting tumor neovascularization. HDAC inhibitors are different from traditional cytotoxic drugs and typical targeted drugs in their mechanism of action. In addition, HDAC inhibitors...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C291/04A61K31/167A61K31/165A61P35/00
Inventor 何彬李燕王芳陈晓雪王春朱红邹叶芳尤玲
Owner GUIZHOU MEDICAL UNIV
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