Ternary conjugates for antineoplastic drugs, compound and application

The invention relates to a target transfer system for an antineoplastic lyophobic drug and mainly relates to E selectin polypeptide ligand-polyethylene glycol-antineoplastic drug conjugates containing disulfide bonds and connected with different link bridges, including compounding of conjugates, ant...

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Bibliographische Detailangaben
Hauptverfasser: GUO NA, TENG YUOU, HAO TIANTIAN, WANG DONG, SHANG XIUZHUAN, LIU HUAN, ZHANG TIANLE, YU PENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a target transfer system for an antineoplastic lyophobic drug and mainly relates to E selectin polypeptide ligand-polyethylene glycol-antineoplastic drug conjugates containing disulfide bonds and connected with different link bridges, including compounding of conjugates, antineoplastic activity evaluation, particle size and morphological characteristics of nanometer particles formed by self-polymerization of the conjugates in aqueous solution and release conditions of antineoplastic drugs under different conditions. The conjugates can actively target to tumor locus blood vessels through E selectin polypeptide ligands and also can self-polymerize into nanometer particles in an aqueous solution so as to be passively targeted to the tumor locus through EPR effect. A result shows that the compounds have obvious antineoplastic activity and low toxicity to normal cells; the compounds can restrain the adhesion of tumor cells and vascular endothelial cells, so that the compounds have the pote