Article-Journal

Molecular editing of bilobalide: Regioselective C-ring lactam formation

Late-stage diversification of complex natural products enables rapid access to analogues for structure-activity relationship studies. Herein, we report a regioselective …

wenjing-wang

Carbohydrate‐based drug discovery: Synthetic strategies and clinical applications

Carbohydrates are integral to drug discovery, serving as versatile templates for the development of small‐molecule therapeutics. However, their success in antiviral, anticancer, …

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Stephan Scheeff

Antiviral profiling and cellular activation of carbobicyclic nucleoside analogues

Nucleoside analogues are important antiviral and anticancer agents. In this study, we investigated a new class of nucleoside analogues built on a synthetically accessible …

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Stephan Scheeff

Ligand-directed self-assembling chimeras for targeted protein O-GlcNAcylation

Precise control of protein-specific O-GlcNAcylation in cells remains a major challenge. Chemically induced proximity (CIP) offers a promising path forward, but its application to …

zhihao-guo

Practical access to trisubstituted Morita‐Baylis‐Hillman‐type products through copper‐catalyzed reductive aldol reactions of alkynones

AbstractWe report a convenient and diastereoselective copper‐catalyzed reductive alkynone aldol addition to aldehydes, with pinacolborane as stoichiometric reductant, that results …

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Stephan Scheeff

Lactone-to-lactam editing alters the pharmacology of bilobalide

Precise transformations of natural products (NPs) can fine-tune their physicochemical properties while preserving inherently complex and evolutionarily optimized parent scaffolds. …

xiaoding-jiang
Diastereo- and enantioselective construction of stereochemical arrays exploiting non-classical hydrogen bonding in enolborates featured image

Diastereo- and enantioselective construction of stereochemical arrays exploiting non-classical hydrogen bonding in enolborates

We report a copper-catalyzed reductive aldol addition to aldehydes and ketones, with pinacolborane as stoichiometric reductant, that results in the generation of stereodefined …

matthew-li
Design and synthesis of bicyclo[4.3.0]nonene nucleoside analogues featured image

Design and synthesis of bicyclo[4.3.0]nonene nucleoside analogues

Nucleoside analogues are effective antiviral agents, and the continuous emergence of pathogenic viruses demands the development of novel and structurally diverse analogues. Here, …

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Stephan Scheeff

Making it hard to replicate

Understanding how to harden liquid condensates produced by influenza A virus could accelerate the development of novel antiviral drugs.

billy-wai-lung-ng

Copper-catalyzed reductive Ireland-Claisen rearrangements of propargylic acrylates and allylic allenoates

The copper-catalyzed reductive Ireland-Claisen rearrangement of propargylic acrylates led to 3,4-allenoic acids. The use of silanes or pinacolborane as stoichiometric reducing …

siyuan-guo