Tumor-targeting dendritic macromolecular paramagnetic metal complex and its synthesis process and use
A paramagnetic metal, tumor-targeting technology, applied in anti-tumor drugs, pharmaceutical formulations, chemical instruments and methods, etc., can solve the problem of non-selectivity or targeting of tissues or organs, short retention time of Magnevist, etc. question
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Embodiment 1
[0094] 6.28g of dendrimer G1 and 5mL of triethylamine were dissolved in 60mL of distilled water, cooled with ice salt at -20°C, and slowly added dropwise with 8.0g of bromoethane-substituted 1,4,7,10-azacyclododecane under stirring. 30ml of dimethylformamide DMF solution of DOTA monosulfonamide, react at low temperature for 4h, rise to room temperature and continue to react for 48h, filter, evaporate part of the solvent under reduced pressure, cool to room temperature, pour the residual solution into 600mL under stirring In the mixed solvent of absolute ethanol-anhydrous ether, the volume ratio of absolute ethanol: anhydrous ether is 1:2, a light yellow precipitate is produced, filtered, and drained, and the resulting solid is dissolved in distilled water, and with absolute ethanol, also It can be reprecipitated with anhydrous ether, and the pale yellow solid is collected and dried in vacuum to obtain 12.1 g of the ligand with a yield of 90%.
[0095] Dissolve 1.34g of the lig...
Embodiment 2
[0097] Sulfadiazine-containing tumor-targeting dendrimer MRI contrast agents.
[0098] a) Reaction of sulfadiazine with phosgene
[0099] Dissolve 1g of sulfadiazine in 20mL of DMF, add 1mL of triethylamine and stir, cool in an ice-water bath, pass phosgene under stirring for 1 hour, stir at room temperature for 2 hours, pass dry air to drive away residual phosgene, and use the reaction solution for later use;
[0100] b) Synthesis of Dendrimer MRI Contrast Agents
[0101] Dissolve 1.4g dendrimer G5 in an appropriate amount of water, add the reaction solution in step a), stir at room temperature for 12 hours, cool in an ice bath, add 4.37g DMF solution of DTPA mono-N-hydroxysuccinimide active ester in batches under stirring , continue to react at 0-5°C for 0.5 hours, then react at room temperature for 24 hours, adjust the pH of the reaction solution to neutral with sodium hydroxide solution, distill off water and most of the DMF under reduced pressure, add 20mL of water to di...
Embodiment 3
[0103] Folic acid-containing tumor-targeting dendrimer MRI contrast agent
[0104] a) Synthesis of folic acid mono-N-hydroxysuccinimide (PGA-OSu)
[0105] Dissolve 1.0g of folic acid (PGA) in 60mL of DMSO, add 1mL of triethylamine, cool in an ice-salt bath, add 0.5g of DCC in batches under stirring, stir for 30 minutes, then add 0.3g of N-hydroxysuccinimide, React for 1 hour, react at room temperature for 24 hours, filter, and store the filtrate in the refrigerator for later use;
[0106] b) Synthesis of Dendrimer MRI Contrast Agents
[0107] 1.2g dendrimer G4 (0.169mmol) was dissolved in 30mL DMF, cooled to -15°C, added 4.2g DTPA monoisobutyl ester solution under stirring, stirred and reacted at -15°C for 1 hour, and reacted at room temperature for 2 hours, in an ice bath Cool, add the DMSO solution of PGA-OSu under stirring, continue to stir the reaction at room temperature for 24 hours, evaporate most of the solvent under reduced pressure, add 20mL of water to dilute, adj...
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