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Application of nitrogen mustard based piperlongumine compound in medicine

A technology of piperonamides and compounds is applied to the application field of nitrogen mustardyl piperonamide compounds in medicine, and can solve problems such as the application of nitrogen mustardyl piperonamide compounds which have not been seen before.

Inactive Publication Date: 2016-03-23
广东永纯医药集团有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] For this reason so far, also do not see the application of nitrogen mustard base perylene amide compound in medicine

Method used

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  • Application of nitrogen mustard based piperlongumine compound in medicine
  • Application of nitrogen mustard based piperlongumine compound in medicine
  • Application of nitrogen mustard based piperlongumine compound in medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Compound DJBB-1 preparation of

[0018] The synthetic route is as follows:

[0019]

[0020] For the synthetic route of intermediate 1, please refer to the reference (Liu Wenhu et al., Acta Pharmaceutica Sinica, 2014, 49(2):217-224).

[0021] For the synthetic route of intermediate 2, please refer to the reference (Shoujiao Pengetal, J. Med. Chem. 2015, 58, 5242? 5255).

[0022] The synthetic route of compound DJBB-1 can be found in the reference (ShoujiaoPengetal, J.Med.Chem.2015, 58, 5242? 5255):

[0023] Add raw material 110mmol, intermediate 210mmol, CH 2 Cl 2 10ml, 10ml of triethylamine, stirred at room temperature for 10h. Then add saturated NH 4 Washed with Cl solution, CH 2 Cl 2 Extraction, washing with saturated brine, MgSO 4 Dried and concentrated. The crude product was separated by column chromatography with a yield of 65%.

[0024] 1 HNMR (400MHz, CDCl 3 ): δ7.89(d,J=15.6Hz,1H),7.60-7.54(m,2H),7.34(d,J=15.6Hz,1H),6.94-6.90(m,3H),6...

Embodiment 2

[0026] Embodiment 2: compound DJBB-2 preparation of

[0027] The synthetic route is the same as compound DJBB-1.

[0028] The yield of compound DJBB-2 was 60%.

[0029] 1 HNMR (400MHz, CDCl 3 ): δ7.90(d,J=15.6Hz,1H),7.32(d,J=15.6Hz,1H),6.96-6.92(m,3H),6.02(t,J=9.6Hz,1H),4.06 (t, J=6.4Hz, 2H), 3.89(s, 6H), 3.86(t, J=7.6Hz, 4H), 3.74(t, J=7.6Hz, 4H), 2.42(m, 2H).

[0030] MS-ESI (m / z): 449.10 (M+Na 十 ).

Embodiment 3

[0031] Embodiment 3: compound DJBB-3 preparation of

[0032] The synthetic route is the same as compound DJBB-1.

[0033] The yield of compound DJBB-3 was 56%.

[0034] 1 HNMR (400MHz, CDCl 3 ): δ7.92(d,J=15.6Hz,1H),7.36(d,J=15.6Hz,1H),6.96-6.92(m,3H),6.03(t,J=9.6Hz,1H),4.03 (t, J = 6.4Hz, 2H), 3.82 (t, J = 7.6Hz, 4H), 3.76 (t, J = 7.6Hz, 4H), 2.46 (m, 2H).

[0035] MS-ESI (m / z): 425.06 (M+Na 十 ).

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Abstract

The invention provides application of a nitrogen mustard based piperlongumine compound in medicine. On the basis of the research on the nitrogen mustard based piperlongumine compound for inhibiting the activity of malignant cells, it proves that the nitrogen mustard based piperlongumine compound has the good anti-tumor activity, and a new choice is provided for preparing anti-tumor medicine.

Description

technical field [0001] The present invention relates to the use of nitrogen mustard amide compounds in medicine, in particular to the application of nitrogen mustard amide compounds in the treatment of malignant tumors. Background technique [0002] Piper longum is a perennial herbaceous vine. Traditional Chinese medicine takes its fruit ears as medicine. It is mainly used for cold pain in the abdomen, vomiting, diarrhea, migraine, nasal sinusitis, external treatment of toothache, coronary heart disease, and angina pectoris. Piperlongumine [0003] It is one of the main active ingredients isolated from Piper longum, and belongs to alkaloid compounds. With the deepening of its research, many pharmacological effects of perylene amide have been discovered. It has many pharmacological activities such as anti-platelet aggregation, analgesia, anti-fungal, anti-schistosome, anti-anxiety and anti-depression. In particular, it exhibits significant cytotoxicity to a variety of tumo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/86A61P35/00A61P35/02
CPCC07D211/86
Inventor 金加明
Owner 广东永纯医药集团有限责任公司
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