Click synthesis of a polyamidoamine dendrimer-based camptothecin prodrug
نویسندگان
چکیده
منابع مشابه
Synthesis, cellular transport, and activity of polyamidoamine dendrimer-methylprednisolone conjugates.
Dendrimers have emerged as promising multifunctional nanomaterials for drug delivery due to their well-defined size and tailorability. We compare two schemes to obtain methylprednisolone (MP)-polyamidoamine dendrimer (PAMAM-G4-OH) conjugate. Glutaric acid (GA) was used as a spacer to facilitate the conjugation. In scheme A, PAMAM-G4-OH was first coupled to GA and then further conjugated with MP...
متن کاملRecent advances in click chemistry applied to dendrimer synthesis.
Dendrimers are monodisperse polymers grown in a fractal manner from a central point. They are poised to become the cornerstone of nanoscale devices in several fields, ranging from biomedicine to light-harvesting. Technical difficulties in obtaining these molecules has slowed their transfer from academia to industry. In 2001, the arrival of the "click chemistry" concept gave the field a major bo...
متن کاملSynthesis of Polyamidoamine Dendrimer for Encapsulating Tetramethylscutellarein for Potential Bioactivity Enhancement
The biomedical potential of flavonoids is normally restricted by their low water solubility. However, little has been reported on their encapsulation into polyamidoamine (PAMAM) dendrimers to improve their biomedical applications. Generation four (G4) PAMAM dendrimer containing ethylenediaminetetraacetic acid core with acrylic acid and ethylenediamine as repeating units was synthesized by diver...
متن کاملSynthesis and Antitumor Properties of BQC-Glucuronide, a Camptothecin Prodrug for Selective Tumor Activation.
Major limitations of camptothecin anticancer drugs (toxicity, nonselectivity, water insolubility, inactivation by human serum albumin) may be improved by creating glucuronide prodrugs that rely on beta-glucuronidase for their activation. We found that the camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC) displays greater cytotoxicity against cancer cells than the clin...
متن کاملPolyamidoamine dendrimer impairs mitochondrial oxidation in brain tissue
BACKGROUND The potential nanocarrier polyamidoamine (PAMAM) generation 5 (G5-NH(2)) dendrimer has been shown to evoke lasting neuronal depolarization and cell death in a concentration-dependent manner. In this study we explored the early progression of G5-NH(2) action in brain tissue on neuronal and astroglial cells. RESULTS In order to describe early mechanisms of G5-NH(2) dendrimer action i...
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ژورنال
عنوان ژورنال: RSC Advances
سال: 2015
ISSN: 2046-2069
DOI: 10.1039/c5ra07987j