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
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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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