Novel type warheads expand toolbox for covalent inhibitors
Synthetic access to strained bicyclobutane sulfonamides enabled the discovery of novel covalent warheads.
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, …
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 …
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
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
Personal Review: International Symposium on Medicinal Chemistry
Synthesis of stasseriolide natural products and their analogues using a ring-closing alkyne metathesis by Alois Fürstner and his team.
Macrocycles can lock the Conformation of Drug Candidates and enhance their Activity
Macrocycles can improve the conformation, biological activity, selectivity, ADME properties, and target affinity of small-molecule drug candidates.
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Synthesis of Drug Libraries using Sulfamide Linker Strategy
A coupling strategy ready for use in a 96 well plate.
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Pfizer's Second-Generation SARS-CoV-2 Protease Inhibitor
Researchers from Pfizer have developed a structurally-optimized SARS-CoV-2 main protease inhibitor with improved metabolic stability compared to nirmatrelvir which is now in …
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Biocatalytic diversification of thionucleoside analogues
Novel biocatalytic method for the diversification of thionucleosides, demonstrating that enzyme-catalyzed transglycosylation can effectively facilitate nucleobase exchange.
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