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A kind of bisarylmaleimide compound and its pharmaceutically acceptable salt as well as its preparation method and application
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A maleimide and compound technology, applied in the field of bisarylmaleimide compounds, can solve problems such as decreased activity and tumors
Inactive Publication Date: 2018-12-11
ZHEJIANG UNIV OF TECH +1
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The above two reasons will make some dioxygenases dependent on α-KG include prolyl hydroxylase (prolyl hydroxylase, PHD), DNA hydroxylase Tet family and histonelysinedemethylase (histonelysine demethylases, KDMs) activity decreased, eventually leading to tumorigenesis
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[0029] Add 2.0g (4.9mmol) 3-(tributyltinyl)-1H-pyrazol[3,4-b]pyridine and 30mL anhydrous DMF into the three-necked flask, control the temperature at 0-5°C, and add 0.22g in batches (5.5mmol) 60% NaH, after adding, keep stirring for 30min, then dropwise add 0.84g (5.9mmol) methyl iodide, react at 0~5°C for 1h after dropping, then rise to room temperature for 0.5h, after the reaction, put The reaction solution was poured into 600mL water, extracted with dichloromethane (50mL×3), the organic layers were combined, washed with saturated brine (150mL×3), dried over anhydroussodiumsulfate, filtered, the filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column Purification by analysis (petroleumether: ethyl acetate = 6:1, v / v) gave 1.56 g of oil 2a with a yield of 75.5%. 1 H NMR (CDCl 3 )δ:0.89(9H,t,J=7.5Hz),1.21-1.26(6H,m),1.33-1.38(6H,m),1.58-1.63(6H,m),4.19(3...
Embodiment 2
[0030] Example 2: 1-Ethyl-3-(tributyltinyl)-1H-pyrazol[3,4-b]pyridine (2b)
[0031] The synthesis method is the same as that in Implementation 1, except that ethyl bromide is used instead of methyl iodide to obtain oil 2b, yield: 62.3%, 1 HNMR (CDCl 3 )δ:0.89(9H,t,J=7.5Hz),1.22-1.27(6H,m),1.34-1.40(6H,m),1.54(3H,t,J=7.5Hz),1.57-1.64(6H ,m),4.63(2H,q,J=7.5Hz),7.04-7.07(1H,m),8.00(1H,dd,J=8.0,1.5Hz),8.50(1H,dd,J=4.5,1.5 Hz).
Embodiment 3
[0032] Example 3: 1-Butyl-3-(tributyltinyl)-1H-pyrazol[3,4-b]pyridine (2c)
[0033] The synthetic method is the same as that in Implementation 1, except that methyl bromide is used instead of methyl iodide to obtain oil 2c with a yield of 58.3%. 1 H NMR (CDCl 3 )δ:0.89(9H,t,J=7.5Hz),0.95(3H,t,J=7.5Hz),1.20-1.29(8H,m),1.32-1.39(8H,m),1.56-1.63(6H ,m),4.57(2H,t,J=7.5Hz),7.03-7.08(1H,m),8.01(1H,dd,J=8.0,1.5Hz),8.50(1H,dd,J=4.5,1.5 Hz).
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Abstract
The invention discloses a bisarylmaleimide compound and its pharmaceutically acceptable salt as well as its preparation method and application, specifically as an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor and its Application in the treatment of malignant tumors such as glioma and acute myeloid leukemia. The bisarylmaleimide compound provided by the invention has highly efficient and selective IDH1 mutant inhibitory activity, and can be used for treating malignant tumors such as glioma and acute myeloid leukemia mediated by IDH1 mutation. The invention has reasonable design and simple and practical preparation method.
Description
technical field [0001] The present invention mainly relates to a kind of bisarylmaleimide compound and its pharmaceutically acceptable salt as well as its preparation method and application. Application in the treatment of malignant tumors such as glioma and acute myeloid leukemia mediated by IDH1 mutation. Background technique [0002] Malignant tumors are one of the major diseases that threaten human health. Worldwide, 8.5 million people died of cancer in 2008, and according to current trends, by 2020 it is expected that there will be 20 million new cancer cases, of which the death toll will reach 12 million. The prevention and treatment of tumors has become an important research topic in the medical circles of various countries. Although people have a deeper understanding of the cause and development of tumors, and a large number of anti-tumor drugs are used clinically. However, these widely used antitumor drugs often have problems such as high toxicity and side effect...
Claims
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