Abstract: Disclosed is a targeted delivery system for a hydrophobic antitumor drug, referring to conjugates of E-selectin polypeptide ligand-polyethylene glycol-antitumor drug connected by different link bridges containing disulfide bonds. The synthesis of the conjugates, antitumor activity evaluation, the particle size and morphology characteristics of nanoparticles self-assembled by the conjugates in an aqueous solution, and the release of the antitumor drug in different conditions are comprised. The conjugates can actively target at vessels of a tumor site by the E-selectin peptide ligand, and can also self-assemble into nanoparticles in an aqueous solution, so as to be passively targeted at the tumor site by EPR effect.

Abstract: Disclosed herein is a preparation method and use of a surface double-modified human serum albumin as a tumor targeting nano drug carrier, wherein the targeting nano drug carrier includes human serum albumin (HSA), polyethylene glycol and E-selectin peptide ligand. The targeting nano drug carrier is formed by coupling the E-selectin peptide ligand and polyethylene glycol to the surface of HSA by thioether linker formed between the sulfhydryl group of E-selectin peptide ligand and activated HSA. The targeting nano drug carrier can encapsulate hydrophobic antitumor drugs and form nanoparticles with certain particle size after treatment, which can not only increase the solubility and stability of the hydrophobic antitumor drugs, but also can actively recognize and bind E-selectin which is highly expressed on activated endothelial cells at tumor site, competitively inhibit the interaction between E-selectin and tumor cells, and thus inhibit the adhesion and migration of tumor cells.

Abstract: A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.

Abstract: A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.

Abstract: Disclosed is a targeted delivery system for a hydrophobic antitumor drug, referring to conjugates of E-selectin polypeptide ligand-polyethylene glycol-antitumor drug connected by different link bridges containing disulfide bonds. The synthesis of the conjugates, antitumor activity evaluation, the particle size and morphology characteristics of nanoparticles self-assembled by the conjugates in an aqueous solution, and the release of the antitumor drug in different conditions are comprised. The conjugates can actively target at vessels of a tumor site by the E-selectin peptide ligand, and can also self-assemble into nanoparticles in an aqueous solution, so as to be passively targeted at the tumor site by EPR effect.