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Indole compound and applications thereof, and pharmaceutical composition and applications thereof
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A kind of compound, technology of indole, applied in indole compound and its application field
Active Publication Date: 2019-01-01
广州智药生物科技有限公司
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Subsequently, through the application of epigenetic screening and targeted biochemistry, some small molecular compounds have been discovered, but there are no compounds that have entered clinical research
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[0075] Ethyl methylpiperidine-4-carboxylate (2 g, 14 mmol) was dissolved in 20 mL of DCM solution, then 2-chloroacetyl chloride (1.16 mL, 15.4 mmol) and K2CO3 (5.8 g, 42 mmol) were added. The reaction system was stirred at room temperature for 5 h. TLC monitoring, after the reaction was completed, 30 mL of water was added, extracted with DCM (3 × 20 mL), the organic phase was washed once with saturated brine, and dried over anhydroussodiumsulfate. The organic phase was spin-dried in vacuo to obtain 2.072 g of a yellow oil (67.4% yield). 1H NMR (400 MHz, CDCl3) δ4.32(m,1H),4.10(m,1H),4.02–3.76(s,3H),3.70(s,2H),3.30–3.14(m,1H), 2.94 (td,J=13.4,2.9Hz,1H),2.70–2.50(m,1H),2.08–1.90(m,2H),1.90–1.61(m,2H).
[0076] (2) Synthesis of QP19 1-(2-(3-acetyl-1H-indol-1-yl)acetyl)piperidine-4-carboxylic acid met...
Embodiment 2
[0079]Synthesis of ethyl 2-(3-acetyl-1H-indol-1-yl) acetate, the synthesis method is as in Example 1. 1H NMR (400MHz, CDCl3) δ8.39 (dd, J=6.4, 2.6 Hz,1H),7.76(s,1H),7.31(dt,J=6.9,3.5Hz,2H),7.26(s,1H), 4.88(s,2H),4.25(q,J=7.1Hz,2H ),1.60(s,3H),1.28(d,J=7.1Hz,3H).
Embodiment 3
[0081] Synthesis of 2-(3-acetyl-1H-indol-1-yl)acetic acid, the synthesis method is as in Example 8. 1H NMR (400MHz, DMSO) δ8.32 (s, 1H), 8.22–8.16 (m, 1H), 7.49(d, J=7.4Hz, 1H), 7.28–7.18(m, 2H), 5.12(s, 2H), 2.44(s, 3H).
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Abstract
The present invention provides an indole compound and applications thereof, wherein the compound can effectively inhibit a CBP / EP300 Bromodomainreceptor, and can be used as a drug for cancers, inflammatory diseases, autoimmune diseases, septicemia and viral infections.
Description
technical field [0001] The invention relates to the technical field of chemistry and medicine, in particular to an indole compound and its application. Background technique [0002] Bromodomains are evolutionarily conserved modules that mediate protein-protein interactions. Bromodomain is a reader of histoneacetylation, which can specifically recognize histone acetylated lysine residues, thereby affecting the transcription and translation of target genes. The abnormal function of this protein complex is related to the occurrence of various diseases, which makes Bromodomain protein become a novel target. Inhibitors of Bromodomain proteins have important biological significance. For example, a large number of compounds have been reported to have curative effects on diseases such as cancer, inflammatory diseases and autoimmune diseases, sepsis, and viral infections. [0003] The Bromodomain protein was named after it was first discovered in a Drosophila gene. Since then, bro...
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