98%
921
2 minutes
20
DNA-encoded libraries (DELs) enable screening of billions of molecules in a single pool through affinity-based selection and have become an indispensable hit finding technology. Although DELs provide relatively easy access to billions of molecules, some methodologies to chemically diversify DELs remain adapted to partially aqueous conditions. To address this challenge, we recently demonstrated the use of surfactant-DNA (Surf-DNA) complexes as an effective approach to facilitate DEL-compatible reactions under anhydrous conditions. Herein, we report the expansion of Surf-DNA to affect an amino radical transfer (ART) coupling for forging challenging C(sp)-C(sp) bonds on DNA with high functional group tolerance over a broad range of substrates. We also report an optimized and simplified Surf-DNA workflow, enabling seamless transition into large-scale DEL productions.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1021/acs.orglett.5c02769 | DOI Listing |
Org Lett
September 2025
State Key Laboratory of Natural Product Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China.
Herein, we report that a novel and efficient bifunctional reagent, benzophenonoxime -(CF) thiocarbonate (BOST), is easily synthesized and successfully applied to the 1, ( ≥ 2)-trifluoromethylthioamination of alkenes under photocatalytic energy transfer conditions. This study not only achieves the radical trifluoromethylthioamination of olefins for the first time but also provides structurally important and diverse SCF-featured amino acid esters and amino nitriles that were previously inaccessible.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
September 2025
Department of Chemistry, Korea University, Seoul, 02841, South Korea.
Chemodynamic therapy (CDT), leveraging Fenton reactions to generate hydroxyl radicals (•OH) from intracellular hydrogen peroxide (HO), offers a promising cancer treatment strategy due to its high specificity and low systemic toxicity. However, the targeted delivery of •OH-producing prodrugs using covalent organic frameworks (COFs) remains a significant challenge. Here, we report a mitochondria-targeted COF-based nano prodrug, COF-31@P, designed for enhanced CDT efficacy.
View Article and Find Full Text PDFChemistry
September 2025
National Engineering Research Center for Carbohydrate Synthesis, Jiangxi Normal University, Nanchang, 330022, China.
We report a glycosyl radical-based, 1,2-trans-selective synthesis of C-aryl glycosides of 2-deoxy-2-amino-sugars from glycals via photoredox PCET/Ni dual catalysis. Mechanistic studies indicate that glycosyl radical formation involves the generation of an N-radical through a proton-coupled electron transfer (PCET) process, followed by its addition to the glycal. This protocol features: a) the use of an inexpensive organic photosensitizer and readily available glycals and aryl bromides; b) good functional group tolerance for both aryl bromides and glycal substrates; c) excellent diastereoselectivity, with exclusive formation of the 1,2-trans C-glycosides in all cases.
View Article and Find Full Text PDFFood Res Int
November 2025
Northeast Agricultural University, College of Food Science, Harbin 150030, PR China. Electronic address:
Sesame protein of different cultivars exhibits varying functional characteristics, making it challenging to achieve standardization in industrial applications. Therefore, we aimed to identify more suitable sesame protein for industrial processing. This study characterized the composition, structure, interfacial properties, and functional traits of sesame protein of nine cultivars.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
September 2025
Materdicine Lab, School of Life Sciences, Shanghai University, Shanghai, 200444, P.R. China.
The stimulator of interferon genes (STING) pathway is a central target in cancer immunotherapy, but current STING agonist therapies lack precision control, leading to suboptimal therapeutic outcomes and systematic adverse effects. Herein, we engineered a dual-locked immuno-polymeric nanoplatform (IPN) with precise spatiotemporal control over the release of STING agonists to enhance cancer immunotherapy. This platform, constructed from biocompatible poly(β-amino esters) (PBAE), incorporates the STING agonist (MSA-2) covalently linked via ester bonds, which is co-assembled with a sonosensitizer.
View Article and Find Full Text PDF