convenient synthesis
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2022 ◽  
Vol 12 ◽  
Yushuai Liu ◽  
Yuanyuan Geng ◽  
Beilei Yue ◽  
Pui-Chi Lo ◽  
Jing Huang ◽  

Cancer immunotherapy can boost the immune response of patients to eliminate tumor cells and suppress tumor metastasis and recurrence. However, immunotherapy resistance and the occurrence of severe immune-related adverse effects are clinical challenges that remain to be addressed. The tumor microenvironment plays a crucial role in the therapeutic efficacy of cancer immunotherapy. Injectable hydrogels have emerged as powerful drug delivery platforms offering good biocompatibility and biodegradability, minimal invasion, convenient synthesis, versatility, high drug-loading capacity, controlled drug release, and low toxicity. In this review, we summarize the application of injectable hydrogels as a unique platform for targeting the immunosuppressive tumor microenvironment.

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 201
István Timári ◽  
Sára Balla ◽  
Krisztina Fehér ◽  
Katalin E. Kövér ◽  
László Szilágyi

Detailed investigation of ligand–protein interactions is essential for better understanding of biological processes at the molecular level. Among these binding interactions, the recognition of glycans by lectins is of particular importance in several diseases, such as cancer; therefore, inhibition of glycan-lectin/galectin interactions represents a promising perspective towards developing therapeutics controlling cancer development. The recent introduction of 77Se NMR spectroscopy for monitoring the binding of a selenoglycoside to galectins prompted interest to optimize the sensitivity by increasing the 77Se content from the natural 7.63% abundance to 99%. Here, we report a convenient synthesis of 77Se-enriched selenodigalactoside (SeDG), which is a potent ligand of the medically relevant human galectin-3 protein, and proof of the expected sensitivity gain in 2D 1H, 77Se correlation NMR experiments. Our work opens perspectives for adding isotopically enriched selenoglycans for rapid monitoring of lectin-binding of selenated as well as non-selenated ligands and for ligand screening in competition experiments.

Yijie Hu ◽  
Xiaoli Wang ◽  
Nan Ren ◽  
Na Li ◽  
Jianyang Li ◽  

Chaithra R. Shetty ◽  
L. Dikshith ◽  
Fathima Sible Dsouza ◽  
Fathimath Shahana ◽  
Fatima Nooha

Chalcone is a simple chemical structure which is present in most of the naturally occurring substances. Many chalcone derivatives are synthesized by Claisen-Schmidt condensation reaction. It is a subject of great research opportunity due to numerous biological activities and convenient synthesis of chalcones. This study aims on synthesizing different α, β unsaturated ketones (chalcones) containing thiophene from thiophene-2-carbaxldehyde and different substituted acetophenones, further evaluating antibacterial activity of synthesized compounds. The synthesized compounds are characterized for their spectral study. From the antibacterial study it was observed that the compounds bearing electron withdrawing group, electron releasing group exhibited excellent to moderate antibacterial activity respectively. These results showed that chalcones incorporated with thiophene have better scopes for further development of the antimicrobial agents.

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7355
Michael T. Shea ◽  
Gregory T. Rohde ◽  
Yulia A. Vlasenko ◽  
Pavel S. Postnikov ◽  
Mekhman S. Yusubov ◽  

Hypervalent iodine heterocycles represent one of the important classes of hypervalent iodine reagents with many applications in organic synthesis. This paper reports a simple and convenient synthesis of benziodazolones by the reaction of readily available iodobenzamides with m-chloroperoxybenzoic acid in acetonitrile at room temperature. The structure of one of these new iodine heterocycles was confirmed by X-ray analysis. In combination with PPh3 and pyridine, these benziodazolones can smoothly react with alcohols or amines to produce the corresponding esters or amides of 3-chlorobenzoic acid, respectively. It was found that the novel benziodazolone reagent reacts more efficiently than the analogous benziodoxolone reagent in this esterification.

2021 ◽  
Vol 16 (1) ◽  
pp. 48-56 ◽  
Xiaolin Zhang ◽  
Nanxin Liu ◽  
Mi Zhou ◽  
Songhang Li ◽  
Xiaoxiao Cai

In recent years, tetrahedral Framework Nucleic Acids(tFNAs) have become a hot topic in the field of DNA nanostructures because of their stable structures, nanoscale size, superior mechanical properties and convenient synthesis with high yield. tFNAs are considered promising drug delivery carriers because they can pass through the cellular membrane without any help and they have a good biocompatibility and biodegradability. Besides, they have rich modification sites, they can be modified by kinds of functional groups. The functionalization molecules can be modified on the vertexes, embedded between the double-stranded DNA of the tetrahedron edges, hanged on the edges, or encapsulated in the cage-like structure of the tetrahedron. The structure of tetrahedron can also be intelligently controlled through smart design, such as integrating DNA hairpin loop structure onto the edges. Nowadays, DNA tetrahedron will have a broader development prospect in the application of drug transport carriers and intelligent drug carriers. Therefore, DNA material is a new carrier material with great advantages and has a very broad application prospect in the construction of an intelligent drug transport system.

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