2,5-Dihydropyrrol-3-yl boron reagents combine a nitrogen-containing five-membered ring with a transformable C–B bond. Through Suzuki–Miyaura coupling, aryl or heteroaryl groups can be introduced at C3, followed by reduction of the double bond to give 3-substituted pyrrolidines. Liashuk et ...
The structures of azaheterocyclic phosphonates can be understood in simplified terms as consisting of a nitrogen-containing ring framework and a phosphonate group directly connected to it through a C–P bond.
Cysteine is one of the amino acid residues most frequently exploited in targeted covalent drug discovery. Its side-chain thiol has substantial nucleophilic potential and can form stable covalent bonds with electrophilic groups such as acrylamides. Targeted covalent inhibitors typically first ...
Dimers formed from two C6–C3 phenylpropanoid units are not limited to C8–C8′ linkages. According to the nomenclature rules of the International Union of Pure and Applied Chemistry (IUPAC), compounds in which two C6–C3 units lack a C8–C8′ bond but are connected through another direct ...
Dengue virus (DENV) mainly comprises four serotypes: DENV-1, DENV-2, DENV-3, and DENV-4. All four serotypes can cause dengue virus infection, but their viral protein sequences are not identical, and the inhibitory activity of the same small molecule may differ substantially among serotypes. ...
Antibody–drug conjugates (ADCs) use tumor cell-surface antigens to achieve antibody recognition and payload delivery. HER2, TROP2, Nectin-4, FRα, and c-Met have received substantial clinical validation, while HER3, B7-H3, CLDN18.2, and DLL3 continue to enter ADC development pipelines. The ...
“Cold” tumors are generally characterized by insufficient tumor antigen presentation, limited effector T-cell infiltration, and pronounced local immunosuppression, resulting in relatively poor responses to immune checkpoint blockade.
Intracellular H₂O₂ and lipid peroxides require the coordinated action of multiple antioxidant enzyme systems for clearance. Among them, Glutathione Peroxidase (GPx), Catalase (CAT), and Peroxiredoxin (PRDX) control peroxides in different substrate and subcellular environments. GPX4 further ...
Taking a typical electrophilic aromatic substitution of pyrrole as an example, the reaction transiently forms a non-aromatic σ-intermediate, followed by deprotonation and restoration of aromaticity. Before and after the reaction, the pyrrole ring remains composed of the original atoms, and the ...
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