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Novel anti-cancer medicaments using NGR(NO2) as targeting carrier, preparation thereof and use thereof

An anti-tumor drug and pharmaceutical technology, applied in the direction of anti-tumor drugs, drug combinations, medical preparations of non-active ingredients, etc., can solve problems such as short metabolic half-life, achieve the effect of reducing toxic side effects and improving targeting

Active Publication Date: 2011-01-19
廖年生 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] In addition, pentafluorouracil is mainly administered by intravenous injection in clinical practice, and its metabolic half-life is very short, only 15 minutes

Method used

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  • Novel anti-cancer medicaments using NGR(NO2) as targeting carrier, preparation thereof and use thereof
  • Novel anti-cancer medicaments using NGR(NO2) as targeting carrier, preparation thereof and use thereof
  • Novel anti-cancer medicaments using NGR(NO2) as targeting carrier, preparation thereof and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0032] 5-FU-NGR (NO 2 The chemical synthesis of:

[0033] 1. Synthetic route:

[0034] 1.1NH 2 -Asn-Gly-Arg (NO 2 ) COOCH 3 Synthesis:

[0035]

[0036] Reagents and conditions: (a) HOBt, DCC, 0°C for 2h and then 8h at r.t.; (b) NH 2 -Gly-OBn TsOH, TEA.; (c) HCl-dry EtOAc.; (d) NH 2 -Arg(NO 2 )-COOCH 3 HCl, TEA.

[0037] 1.2.5-Fu-linker-Asn-Gly-Arg (NO 2 )-COOCH 3 Synthesis:

[0038]

[0039] Scheme 2. (a) 60℃.; (b) DCC, DMAP, dry THF.; (c) 10% Pd / C, AcOH, 1,4-cyclohexene.; (d) pentafluorophenol, EDAC, dry DMF.; (e) TEA, dry THF.

[0040] 2 synthesis method

[0041]Synthesis of Boc-protected asparagine-glycine benzyl ester Boc-Asn-Gly-OBn: 8.25 g (50 mmol) of Boc-protected asparagine was dissolved in 250 ml of anhydrous THF, and then 6.75 g (50 mmol) was added ) of HOBt and 10.3 g (50 mmol) of DCC, the mixed solution was stirred under ice bath for 1 hour, then the ice bath was removed, and the reaction was continued for 6 hours. An anhydrous tetrahydrofur...

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Abstract

The invention provides novel anti-cancer precursor medicaments using NGR(NO2) as a targeting carrier. The novel anti-cancer precursor medicaments are prepared by designing and synthesizing a 5-fluorouracil precursor medicament, a lenalidomide precursor medicament, a cytarabine precursor medicament, an epirubicin precursor medicament and a dasatinib precursor medicament. According to the initial research on the anti-tumor activity of the 5-fluorouracil precursor medicament, the 5-fluorouracil precursor medicament can inhibit the invasion and metastasis of tumor cells and the growth of solid tumors. The 5-fluorouracil precursor medicament is modified in both effectiveness and preparation compared with the 5-fluorouracil serving as a parent medicament and is widely applicable. Concretely, the invention mainly relates to three aspects: (1) design and antiangiogenic effect of a novel tumor-targeted tripeptide NGR(NO2); (2) preparation of anti-cancer precursor medicaments by coupling the tumor-targeted tripeptide NGR(NO2) and 5 anti-cancer medicaments through covalent bonds; and (3) antitumor and antiangiogenic medical use of the novel 5-fluorouracil precursor medicament.

Description

technical field [0001] The invention relates to a novel class of tumor targeting drug carrier NGR (NO 2 ) design, synthesis and specific anti-cancer application, 5 kinds of NGR (NO 2 ) is the design, synthesis, antitumor activity and application of new anticancer drugs as targeting carriers. technical background [0002] Aminopeptidase N (CD13) and NGR tripeptide [0003] Aminopeptidase N (APN / CD13) is a zinc ion-dependent type II metallo-exopeptidase belonging to the M1 aminopeptidase family. Its physiological function is to participate in the degradation of N-terminal amino acids of substrate proteins. Studies have shown that aminopeptidase N is a multifunctional enzyme with a wide range of substrates, and it plays an important role in tumorigenesis, immune function regulation, viral infection and analgesia. Especially in the neovascularization of tumor tissue, APN has a high level of expression, and it plays an important role in the process of tumor angiogenesis and t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/093A61K38/06A61K47/42A61P35/00A61K47/18
Inventor 徐文方栾业鹏廖年生
Owner 廖年生
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