487-66-1Relevant articles and documents
Synthetic Studies on Tautomycin Synthesis of 2,3-Disubstituted Maleic Anhydride Segment
Naganawa, Atsushi,Ichikawa, Yoshiyasu,Isobe, Minoru
, p. 8969 - 8982 (1994)
The 2,3-disubstituted maleic anhydride segment of tautomycin has been synthesized in optically active form.Oxidation of 3,4-disubstituted furan employing singlet oxygen completes the construction of the maleic anhydride moiety.Esterification of the maleic anhydride segment without protecting anhydride moiety resulted in the successful coupling reaction with fragment derived from tautomycin.
A medusa-like β-cyclodextrin with 1-methyl-2-(2'-carboxyethyl) maleic anhydrides, a potential carrier for pH-sensitive drug delivery
Kang, Sunyoung,Park, Euddeum,Kim, Youngeun,Lee, Seonju,Kwon, Jiwoong,Cho, Hyungdo,Lee, Yan
, p. 658 - 668 (2014)
We developed a new pH-sensitive drug delivery carrier based on β-cyclodextrin (β-CD) and 1-methyl-2-(2'-carboxyethyl) maleic anhydrides (MCM). The primary hydroxyl groups of β-CD were successfully attached to MCM residues to produce a medusa-like β-CD-MCM. The MCM residue was conjugated with cephradine (CP) with high efficiency (>90%). More importantly, β-CD-MCM-CP responded to the small pH drop from 7.4 to 5.5 and released greater than 80% of the drugs within 0.5h at pH 5.5. In addition, the inclusion complex between β-CD-MCM-CP and the adamantane derivative was formed by simple mixing to show the possibility of introducing multi-functionality. Based on these results, β-CD-MCM can target weakly acidic tissues or organelles, such as tumours, inflammatory tissues, abscesses or endosomes, and be easily modified with various functional moieties, such as ligands for cell binding or penetration, enabling more efficient and specific drug delivery.
Nano clustering enzyme with hypoxia activation prodrug and preparation method and application of enzyme
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Paragraph 0095-0097, (2019/08/20)
The invention provides a nano clustering enzyme with a hypoxia activation prodrug. The nano clustering enzyme has capacity of targeted tumor hunger and hypoxia activation and is a mode for cancer treatment through cooperation of a chemotherapy and metabolic treatment. An adopted cross-linking agent material polyethylene glycol-b-poly(2-hydroxyethyl methacrylate)segmented copolymer modified by 2-carboxyethyl cellulose-3-methyl maleic anhydride has the acidity response characteristic and can have specificity in tumor targeting breaking. The nano clustering enzyme takes a bovine serum albumin-hypoxia activation drug as a shell, the bovine serum albumin has good biocompatibility and stability so that the nano clustering enzyme can stably exist in the blood, the blood circulation time is prolonged, and the tumor gathering effect is improved. Through the shell, advanced exposure of the enzyme in a core can be avoided, and the toxicity to the normal tissue is lowered. The nano clustering enzyme has good stability and dispersity and is beneficial to biological application.
Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA
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Page/Page column 35; 36, (2016/02/29)
The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinet