Anti-tumor tree-shaped polypeptide macromolecule medicament carrier system
A macromolecular carrier and anti-tumor drug technology, applied in the field of dendritic polypeptide macromolecular drug carrier system, can solve the problems of limited use, non-specific toxicity, poor water solubility, and no treatment options for cancer with chemotherapy drugs
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Examples
Embodiment 1
[0020] Example 1 Synthesis of second-generation glutamic acid dendrimer-camptothecin (1a)
[0021] A suspension of the second-generation glutamic acid dendrimer (300mg, 2.9mmol) and (S)-10-tert-butoxycarbonylcamptothecin (200mg, 0.46mmol) in dimethylformamide (40mL), Dissolution was carried out with gentle heating. When the obtained solution was cooled to room temperature, a solution of chloromethylpyridinium iodide (150 mg, 0.7 mmol) in dimethylformamide (2.5 mL) and 4-dimethylaminopyridine (100 mg, 0.9 mmol) were added sequentially. ) in dimethylformamide (2.5 mL). After stirring for 100 h, the mixture was cooled in an ice bath, then 10% aqueous sodium chloride solution (100 mL) was added within 30 min under vigorous stirring. After acidification to pH = 2 by slowly adding 0.5M hydrochloric acid, it was stirred at room temperature for another 30 min. The solid was collected by centrifugation and the supernatant removed. The solid was suspended in water (200 mL) and isolat...
Embodiment 2
[0023] Example 2 Synthesis of second-generation glutamic acid dendrimer-alanine-camptothecin (2a)
[0024] In the To a suspension in anhydrous dimethylformamide (15 mL), a solution of 1,3-diisopropylcarbodiimide (70 mg, 0.5 mmol) in dimethylformamide (1 mL) was added within 20 min . The mixture was stirred under nitrogen for 2 days. After cooling in an ice bath, 10% aqueous sodium chloride (40 mL) was added within 30 min. After stirring for 1 h, the mixture was adjusted to pH=2.5 by adding 1N hydrochloric acid. The solid was filtered off, washed with water (5 x 25 mL), and dried under vacuum. The solid was washed with 2% methanol-dichloromethane (4 x 50 mL) and dried under vacuum to yield the second-generation glutamic acid dendrimer-alanine-camptothecin (2a) (630 mg, Yield 75%), H-NMR (300MHz, TFA-d): δ 9.45 (s), 7.85-8.6 (m, aromatic hydrocarbon proton), 5.92 (d, J=18.3Hz, lactone proton), 5.70 (s ), 5.62 (d, J=18.3Hz, lactone proton), 4.8 0-6.05 (m), 3.80-4.50 (m), 1....
Embodiment 3
[0026] Example 3 Synthesis of second-generation glutamic acid dendrimer-Gln-Ser-camptothecin (3a)
[0027] The second-generation glutamic acid dendrimer-Gln-Ser-camptothecin (3a) was synthesized from the third-generation glutamic acid dendrimer and O-(N-tert-butoxycarbonyl)Gln-Ser-camptothecin The preparation process is the same as that of 2a.
[0028] Synthesis of three generations of glutamic acid dendrimers-Gln-Ser-camptothecin (3b) and 3a.
PUM
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com