Imidazole peptide deformylase inhibitor with anti-tumor effect

A peptide deformylase and inhibitor technology, which is applied in medical preparations containing active ingredients, antineoplastic drugs, organic chemistry, etc., can solve problems such as shortage of treatment methods, and achieve novel structure, good application prospects, and low toxicity Effect

Pending Publication Date: 2022-07-05
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the clinical methods for treating malignant tumors mainly include surgical resection, chemotherapy and radiotherapy, a...

Method used

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  • Imidazole peptide deformylase inhibitor with anti-tumor effect
  • Imidazole peptide deformylase inhibitor with anti-tumor effect
  • Imidazole peptide deformylase inhibitor with anti-tumor effect

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Example 1 Imidazole peptide deformylase inhibitor and its synthesis method

[0034] 1. The imidazole peptide deformylase inhibitor of this embodiment has the structure shown in formula (1), formula (2) or formula (3):

[0035]

[0036] In formula (1), R 1 selected from hydrogen, halogen, alkyl and cycloalkyl, aromatic or heteroaromatic;

[0037] In formula (2), R 2 is selected from hydrogen, alkyl, cycloalkyl or aryl;

[0038] In formula (3), X is selected from oxygen or sulfur, R 3 is a halogen atom or a benzene ring.

[0039] Specifically, the imidazole peptide deformylase inhibitors in this embodiment include a total of 31 compounds, of which compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23 belong to the structure shown in formula (1); compounds 24, 25, 26, 27, 28 belong to the structure shown in formula (2); compound 29, 30 and 31 belong to the structures represented by formula (3); the structural formulas and mole...

experiment example 2

[0290] Experimental Example 2 Determination of the inhibitory activity of imidazole peptide deformylase inhibitors (compound 1-31) on tumor cells

[0291] 1. Tumor cells used in the test: human colon cancer cells (HCT116) (purchased from Guangzhou Saiku Biotechnology Co., Ltd.), human non-small cell lung cancer cells (A549) (purchased from Guangzhou Saiku Biotechnology Co., Ltd.), human breast Cancer cells (MCF-7) (purchased from Wuhan Prosser Life Technology Co., Ltd.).

[0292] 2. Test method: The CCK-8 method was used to determine the proliferation inhibitory effect of imidazole peptide deformylase inhibitors (compounds 1-31) on human colon cancer cells, human non-small cell lung cancer cells and human breast cancer cells. The process is as follows:

[0293] (1) The above tumor cell lines were prepared into single cell suspensions with the corresponding complete medium, the concentration of the single cell suspension was 50,000 cells / mL, and 100 μL of the cell suspension w...

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Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to an imidazole peptide deformylase inhibitor with an anti-tumor effect. In order to research and develop a novel small molecule compound targeting HsPDF, the invention discloses an imidazole peptide deformylase inhibitor with an anti-tumor effect, and the imidazole peptide deformylase inhibitor is novel in structure, better in activity and small in toxicity, has better anti-tumor activity, and can be used for preparing an anti-tumor drug. The compound has good inhibitory activity on various tumor cells (such as colorectal cancer cells, breast cancer cells and lung cancer cells), can be applied to preparation of anti-tumor drugs or drugs for inhibiting tumor cell proliferation, and has good application prospects in the anti-tumor aspect.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an imidazole peptide deformylase inhibitor with antitumor effect. Background technique [0002] Malignant tumors have always been one of the major diseases that seriously threaten human life and health in the current society. Although with the rapid development of medical science and technology, new therapeutic drugs and treatment methods are constantly emerging, but due to changes in living environment and life pressure, the probability of cancer in the whole society is getting higher and higher, and it is getting younger and younger. Society and family come with a serious burden. According to the 2020 World Statistical Report, about 19.29 million people worldwide suffer from tumors, and there are 9.96 million deaths from cancer worldwide. The incidence and mortality of cancer are still increasing. At present, the main clinical methods for the treatment of mali...

Claims

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Application Information

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IPC IPC(8): C07D487/04C07D233/64C07D263/14C07D277/30A61P35/00A61K31/5377A61K31/4439A61K31/4188A61K31/4709A61K31/4164A61K31/421A61K31/426
CPCC07D487/04C07D233/64C07D263/14C07D277/30A61P35/00C07B2200/07
Inventor 钱宇黄佳武石茂清张中辉张恬源胡文浩
Owner SUN YAT SEN UNIV
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