1301708-62-2Relevant academic research and scientific papers
Peptide-targeted dendrimeric prodrugs of 5-aminolevulinic acid: A novel approach towards enhanced accumulation of protoporphyrin IX for photodynamic therapy
Tewari,Dondi,Yaghini,Pourzand,MacRobert,Eggleston
, (2021)
Photodynamic therapy (PDT) is a promising approach for the targeted treatment of cancer and various other human disorders. An effective, clinically approved approach in PDT involves the administration of 5-aminolevulinic acid (ALA) to generate elevated levels of the natural photosensitiser protoporphyrin IX (PpIX). The development of prodrugs of ALA is of considerable interest as a means to enhance the efficiency and cell selectivity of PpIX accumulation for PDT applications. In this work a novel peptide-targeted dendrimeric prodrug of 5-aminolevulinic acid (ALA) 13 was synthesised which displays nine copies of ALA on a core structure that is linked to a homing peptide for targeted delivery to a specific cancer cell type. The synthesis was accomplished effectively via a flexible, modular solid phase and solution phase route, using a combination of solid phase peptide synthesis and copper-catalysed azide-alkyne cycloaddition chemistry. The prodrug system shows a sustained and enhanced production of protoporphyrin IX (PpIX) in the MDA-MB-231 cell line that over-expresses the epidernal growth factor receptor (EGFR+) in comparison to equimolar ALA and the corresponding non-targeted ALA dendrimer (nine copies of ALA). This study provides a proof of concept for the development of a new generation of prodrugs for ALA-based photodynamic therapy that can deliver an enhanced ALA payload to specific tissue types.
GOLD NANOPARTICLES AND METHODS OF MAKING AND USING GOLD NANOPARTICLES
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Paragraph 0147; 0285, (2015/12/30)
Disclosed herein are embodiments of gold nanoparticles and methods of making and using the gold nanoparticles. The disclosed gold nanoparticles have core sizes and polydispersities controlled by the methods of making the gold nanoparticles. In some embodiments, the methods of making the gold nanoparticles can concern using flow reactors and reaction conditions controlled to make gold nanoparticles having a desired core size. The gold nanoparticles disclosed herein also comprise various ligands that can be used to facilitate the use of the gold nanoparticles in a variety of applications.
Efficient multigram synthesis of the repeating unit of gallic acid-triethylene glycol dendrimers
Amaral, Sandra P.,Fernandez-Villamarin, Marcos,Correa, Juan,Riguera, Ricardo,Fernandez-Megia, Eduardo
supporting information; experimental part, p. 4522 - 4525 (2011/10/08)
A multigram synthesis of the repeating unit of GATG (gallic acid-triethylene glycol) dendrimers is described through an efficient and cost-effective route. These conditions overcome major problems precluding scaling up and afford product in excellent overall yield and purity. Special attention has been paid in this process to green chemistry principles: atom economy, safety, and waste reduction. This scheme could be easily adapted for the preparation of similar dendritic systems.
