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Glycocalixarenes and their affinity to human galectins
Bálková, Denisa ; Bojarová, Pavla (advisor) ; Kavan, Daniel (referee)
Calix[n]arenes are macrocyclic compounds synthesized by the oligomerisation of phenol and formaldehyde. They can have different numbers of phenol rings and can adopt various conformations. As they can be easily modified, they are widely used in many ways, especially in industry or medicine. Modifications can comprise many functional groups such as hydroxyl, amine or carboxyl. Moreover, they can be functionalized with carbohydrates. In such a case, glycocalyx[n]arenes are formed. Galectins, S-type lectins, are capable of specific recognition and subsequent binding of a number of glycoconjugates. However, it is possible only when the molecule presents β-D-galactosides. Galectins have different binding affinities to particular ligands. It has been proven that if the β-D-galactosides are conjugated to a multivalent carrier, galectins have higher affinity to the resulting glycoconjugate. With these ligands it is possible to affect many functions of galectins such as cell adhesion, regulation of apoptosis, proliferation, cell signalling pathways and immune response. Through these pathways, galectins can also cause serious diseases such as autoimmune diseases or carcinogenesis. Thus, the goal of many studies is to find such galectin ligands that could prevent these disorders or help with their treatment....
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Efficient one-pot synthesis of polysubstituted 6-[(1H-1,2,3-triazol-1-yl)methyl]uracils through the "click" protocol
Jansa, Petr ; Špaček, Petr ; Holý, Antonín ; Votruba, Ivan ; Janeba, Zlatko
Synthesis of triazoloacyclic nucleosides and nucleoside phosphonates was developed as the one-pot Cu(I)-catalyzed azide alkyne Huisgen "click" cycloaddition. A novel Cu(I)-catalyzed decarboxylation reaction of 1-substituted 1H-1,2,3-triazole-4-carboxylates at room temperature was observed and used for the preparation of 1-substituted 1H-1,2,3-triazoles.
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