10.1055/s-0031-1291135
The study focuses on the copper-catalyzed 1,3-dipolar cycloaddition of (arylselanyl)alkynes with benzyl azides, producing a series of novel [(arylselanyl)alkyl]-1,2,3-triazoles. This reaction, known as click chemistry, was performed under mild conditions using copper(II) acetate monohydrate and sodium ascorbate as catalysts. Various substituted benzyl azides, both electron-withdrawing and electron-donating, were reacted with different (arylselanyl)alkynes, yielding high amounts of selenium-containing triazoles. The synthesized compounds show potential for biological applications, expanding the utility of selenium-containing heterocycles in organic chemistry.
10.1039/b905938e
The research investigates the creation and binding affinity of multivalent ligands for the Syk tandem SH2 domain using ITAM-derived phosphopeptides attached to dendrimers. The purpose is to enhance the binding affinity of these ligands through multivalency, which could have therapeutic implications for conditions like allergic responses. The researchers synthesized a series of dendrimers with varying valencies (from monovalent to octavalent) by attaching a tetrapeptide sequence (pTyr-Glu-Thr-Leu) from the ITAM motif to dendrimers using 'click' chemistry. The binding affinity of these dendrimers for Syk tSH2 was assessed via surface plasmon resonance (SPR) competition experiments. The study found that tetravalent and octavalent dendrimers exhibited a significant multivalency effect, with affinities in the high nanomolar range, approximately 100-fold enhanced compared to the monovalent tetrapeptide. The key chemicals used include the ITAM-derived phosphopeptide, various generations of dendrimers, copper(I) sulfate, sodium ascorbate for the 'click' chemistry, and Syk tSH2 for binding assays. The conclusion is that multivalency significantly enhances the binding affinity, and further improvements might be achieved by optimizing the orientation of the phosphopeptides on the dendrimers.
10.1021/ol702370m
The research describes the synthesis of monofunctional curcumin derivatives, a "clicked" curcumin dimer, and a PAMAM dendrimer-curcumin conjugate for therapeutic applications. The purpose of this study was to overcome the poor water and plasma solubility of curcumin, a bioactive compound found in turmeric, which possesses antioxidant, anticancer, anti-inflammatory, and anti-Alzheimer's disease properties. The researchers developed a synthetic methodology to produce curcumin conjugates with water-soluble polymers and targeting proteins, potentially enhancing curcumin's therapeutic efficacy. Key chemicals used in the process include curcumin, glutaric anhydride, amino-PEG azide, 1,3-dicyclohexylcarbodiimide (DCC), propargyl bromide, K2CO3, and copper(II) sulfate with sodium ascorbate for the "click" reaction. The study concluded that the monofunctional curcumin derivatives retained biological activity, efficiently labeled and dissolved amyloid fibrils, and the curcumin dimer selectively destroyed human neurotumor cells, making it a promising drug candidate. The conjugates were also expected to exhibit the EPR effect, enhancing their potential therapeutic applications.
