Cyclopeptide antitumor active compound and preparation method and application thereof

An anti-tumor activity, cyclic peptide technology, applied in the field of medicine, can solve the problems of poor membrane permeability, unstable conformation of anti-cancer drugs, weak anti-hydrolase ability, etc., to improve anti-tumor activity, improve enzyme stability and Antitumor activity, the effect of enhancing cell permeability
CN112778403AActive Publication Date: 2021-05-11SHANGHAI UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI UNIV
Publication Date
2021-05-11

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Abstract

The invention relates to the technical field of medicines, and discloses a cyclopeptide antitumor active compound, and particularly relates to a cyclopeptide active molecule with a structure shown in a formula (I), the cyclopeptide active molecule with the structure shown in the formula (I) and pharmaceutically acceptable salt or ester thereof: GFKX1LLKX2X3AKX4LVKX5VLF.NH2(I), wherein X1 represents aspartic acid or (2R)-2-amino-2-methyl-6-heptenoic acid; X2 represents glycine or (2R)-2-amino-2-methyl-6-heptenoic acid; X3 represents alanine or (2R)-2-amino-2-methyl-9-decenoic acid; X4 represents alanine or (2R)-2-amino-2-methyl-6-heptenoic acid; X5 represents threonine or (2R)-2-amino-2-methyl-6-heptenoic acid; and paired (2R)-2-amino-2-methyl-6-heptenoic acid or (2R)-2-amino-2-methyl-9-decenoic acid in a fragment is cyclized through an olefin metathesis reaction. The cyclopeptide antitumor active compound and a preparation method and application thereof aim to enhance the cell permeability and improve the enzyme stability and antitumor activity.
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Description

technical field

[0001] The invention relates to the technical field of medicine, in particular to a cyclic peptide anti-tumor active compound and its preparation method and application. It has the activity of inhibiting the prostate cancer bone metastases cell line C4-2B and can be used to prepare related anti-cancer drugs. Background technique

[0002] Prostate cancer is the most common cancer that occurs in men. Treatment for prostate cancer usually involves surgery, chemotherapy, and androgen deprivation therapy. However, these effective treatments are limited by drug resistance and cytotoxicity. In recent years, small-molecule drugs have been widely used in the treatment of major diseases such as tumors, but small-molecule drugs are also limited due to their large side effects and easy drug resistance. Peptide drugs have low toxicity and high antitumor activity, so they have received extensive attention.

[0003] Ascaphin-8 (GFKDLLKGAAKALVKTVLF.NH2) is an α-helical ant...

Claims

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