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Polyethylene glycol modified anti-tumor prodrug as well as preparation method and application thereof
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A polyethylene glycol and prodrug technology, applied in the field of doxorubicin prodrug and its preparation, can solve the problem of entering tumor tissue and the like, and achieve the effects of simple operation, environmental friendliness and excellent release behavior
Pending Publication Date: 2022-04-01
长沙创新药物工业技术研究院有限公司
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[0008] In view of the above-mentioned technical problem that doxorubicin cannot selectively enter tumor tissue, the present invention provides a polyethylene glycol-doxorubicin prodrug compound containing a novel linker arm and its preparation based on the design concept of the prodrug method, the prodrug has excellent selective sustained-release behavior, and the prodrug and its preparation method have good application prospects
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Embodiment 1
[0085] Embodiment 1: the preparation of intermediate 2a
[0086]
[0087] Put tert-butyl carbazate (2g, 1eq), succinic anhydride (1eq) and water (15mL) in a 100mL round bottom flask and stir at room temperature for 5h. Freeze-dried to obtain compound 2a, a total of 3.5 g, with a yield of 98%.
[0088] 1 H NMR (400MHz, CDCl 3 )δ8.72(s,1H),7.35(s,1H),2.69(t,J=6.7Hz,2H),2.54(t,J=6.7Hz,2H),1.45(s,9H).
Embodiment 2
[0089] Embodiment 2: the preparation of intermediate 2b
[0090]
[0091] Put tert-butyl carbazate (2g, 1eq), glutaric anhydride (1eq) and water (15mL) in a 100mL round bottom flask and stir at room temperature for 5h. Compound 2b was freeze-dried to obtain 3.7 g in total, with a yield of 98%.
[0093] Embodiment 3: the preparation of intermediate 2c
[0094]
[0095] Put tert-butyl carbazate (2g, 1eq), adipic anhydride (1eq) and water (15mL) in a 100mL round bottom flask and stir at room temperature for 5h. Compound 2c was freeze-dried to obtain 3.7 g in total, with a yield of 95%.
[0096] 1 H NMR (400MHz, CDCl 3 )δ8.76(s,1H),7.19(d,J=3.4Hz,1H),2.49(t,J=6.7Hz,2H),2.37(t,J=6.7Hz,2H),1.88–1.99( m,2H),1.73–1.62(m,2H),1.46(s,9H).
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Abstract
The invention relates to a polyethylene glycol modified doxorubicinprodrug as well as a preparation method and application thereof, and belongs to the technical field of biological pharmacy. The polyethylene glycol modified doxorubicinprodrug contains a novel connecting arm of a hydrazide fragment connected by a piperazine heterocyclic ring, the prodrug has an excellent selective slow release behavior, and the preparation method of the prodrug has the advantages of mild reaction conditions, high yield, simplicity and convenience in operation and environmental friendliness. The polyethylene glycol modified doxorubicin prodrug disclosed by the invention has a good application prospect.
Description
technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and in particular relates to a polyethylene glycol-modified doxorubicin prodrug and its preparation method and application. Background technique [0002] Doxorubicin (DOX) is an efficient and broad-spectrum antitumor drug that can inhibit the synthesis of RNA and DNA, and has inhibitory effects on tumor cells of various growth cycles, and is suitable for liver cancer, gastric cancer, acute leukemia and malignant tumors. Lymphoma treatment. However, DOX is highly lethal to tumors, but its selectivity is poor, and it will cause toxic and side effects on normal tissues and organs such as liver, liver, and kidneys. Long-term use will cause strong allergic reactions, cardiotoxicity, and liver damage, and it is easy to produce Sexual multidrug resistance limits the clinical use of doxorubicin to a certain extent. [0003] Polyethylene glycol (PEG) is a synthetic polymer with excellent bioc...
Claims
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