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54results about How to "Improve targeting selectivity" patented technology

Substituted porphyrin gold (III) compounds with anticancer activity and preparation method thereof

The invention discloses substituted porphyrin gold (III) compounds with anticancer activity and a preparation method thereof, belonging to the technical field of medicament preparation. The preparation method comprises the following steps of: coordinating substituted tetraphenylporphyrin and gold to generate a substituted tetraphenyl porphyrin gold (III) compound; and introducing a targeting group onto a porphyrin ring to enhance the targeting selectivity of porphyrin gold, lower the toxicity of the porphyrin gold, further improve the performance of the porphyrin gold (III) compound and preserve or enhance the anticancer activity of the porphyrin gold (III) compound. As proved by in-vitro detection data of an S180 cell, the compound synthesized with the method has a remarkable suppressingfunction, the highest suppression ratio up to 92.863 percent higher than that of tetraphenyl porphyrin gold (III) serving as a lead compound and a weak suppressing function on normal cells. The preparation method is scientific and reasonable; and the prepared substituted porphyrin gold (III) compounds have high anticancer activity, a small toxic or side effect and a simple, convenient, and practical preparation process, and is suitable for industrial mass production.
Owner:YANGZHOU UNIV

Biotin-podophyllotoxin esterified derivative and pharmaceutical composition thereof, as well as preparation methods and applications of derivative and pharmaceutical composition

The invention provides a biotin-podophyllotoxin esterified derivative represented as the general formula (I), pharmaceutical composition taking compounds as active ingredients, as well as applications of the biotin-podophyllotoxin esterified derivative in preparing antitumor drugs and inhibitors. Activity screening proves that the biotin-podophyllotoxin esterified derivative represented as the general formula (I) has better antitumor activity. Meanwhile, a preparation method of the compounds is provided and comprises the following steps: podophyllotoxin is taken as a lead compound, structures of hydroxyl at the 4 site and methoxyl at the 4' site are modified, and a series of compounds are synthesized through connection of different chains between biotin and podophyllotoxin. According to the invention, biotin which is necessary for cell growth is used for structure modification on podophyllotoxin, cancer cell targeting selectivity of a modifier is improved, selective distribution toward cancer cells is realized, and better treatment effect can be achieved. Meanwhile, biotin is soluble in water, and the water solubility problem of drugs can be solved by introducing biotin into podophyllotoxin molecules.
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI

EGF (epidermal growth factor) ligand targeted nano drug-loaded system and anti-tumor treatment application thereof

The invention discloses an EGF (epidermal growth factor) ligand targeted nano drug-loaded system and an anti-tumor treatment application thereof. According to the drug-loaded system, superparamagnetic nanoparticles are taken as magnetic nuclei, carboxymethyl chitosan is taken as a coating material, an anti-tumor drug is transferred to the coating layer, and the carboxymethyl chitosan surface is modified with an EGF. The EGF ligand targeted nano drug-loaded system has the characteristics of good biocompatibility, high stability, good slow release performance and specific target performance, so that the system has high targeted selectivity on tumor cells, can directionally release a drug to a tumor location, then plays roles of targeted inhibition and tumor cell killing and improves the bioavailability of the drug, and a new strategy is provided for targeted therapy of tumors; a preparation method of nano-carriers and the nano drug-loaded system is simple and convenient to operate, reaction conditions are mild, a prepared product can be taken as a wide carrier for the anti-tumor drug, and a new development direction is provided for study of the efficient anti-tumor drug targeted delivery carrier.
Owner:HENAN UNIVERSITY OF TECHNOLOGY
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