ReviewRSC medicinal chemistry2023
Nitriles: an attractive approach to the development of covalent inhibitors.
Review in RSC medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed.
- Next-generation Janus kinase inhibitors: Integrating synthetic innovation, structural biology, and computational design for precision drug discovery.Pharmaceutical science advances · 2026Review
- Photocatalytic Decyanative Borylation of Dicyanoarenes Enabled by Radical-Radical Coupling.Organic letters · 2026Article
- Discovery and Biosynthesis of Nitrilobacillins by Post-Translational Introduction of C-Terminal Nitrile Groups.Journal of the American Chemical Society · 2026Article
- A general synthesis of nitriles from nitroalkanes with bis(catecholato)diboron.Chemical science · 2026Article
- Expedient Discovery of a Metallaphotoredox Cyanomethylation for Synthesizing α-Aryl Nitriles.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Substrate-Affinitive P-Type Azapolycyclic Photosensitizer for Chemoselective Nitrilization Under Mild Conditions.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Discovery and Biosynthesis of Nitrilobacillins by Post-translational Introduction of C-Terminal Nitrile Groups.bioRxiv : the preprint server for biology · 2026Article
- Synthesis, computational studies, and biological evaluation of novel cyanoacrylamides as potential anticancer agents.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Deoxycyanation of Alkyl Alcohols Using Photoredox Catalysis.Organic letters · 2026Article
- Attempts to Achieve Targeted Covalent Inhibition of Hsp90β.Chemical biology & drug design · 2026Article
- Synthesis and preclinical evaluation of FAP-targeting radiotracers for PET and optical imaging.EJNMMI radiopharmacy and chemistry · 2025Article
- Noncovalent interaction-driven regio- and enantioselective hydroalkynylation of unactivated alkenes to access remote chiral nitriles.Science advances · 2025Article
- Evaluating the protonation state of the catalytic Cys25 in cruzain cysteine protease: A target for Chagas disease.Protein science : a publication of the Protein Society · 2025Article
- A Comprehensive Review of Radical-Mediated Intramolecular Cyano-Group Migration.Molecules (Basel, Switzerland) · 2025Review
- Recent advances in focal adhesion kinase (FAK)-targeting antitumor agents.RSC advances · 2025Review
- Potent and Selective Human 5-HTJournal of medicinal chemistry · 2024Article
- Correlating Predicted Reactivities with Experimental Inhibition Data of Covalent ChlaDUB1 Inhibitors.ACS medicinal chemistry letters · 2024Article
- Advances in the Search for SARS-CoV-2 MPathogens (Basel, Switzerland) · 2024Review
- Review
- The Nitrile Bis-Thiol Bioconjugation Reaction.Journal of the American Chemical Society · 2024Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nitriles have broad applications in medicinal chemistry, with more than 60 small molecule drugs on the market containing the cyano functional group. In addition to the well-known noncovalent interactions that nitriles can perform with macromolecular targets, they are also known to improve drug candidates' pharmacokinetic profiles. Moreover, the cyano group can be used as an electrophilic warhead to covalently bind an inhibitor to a target of interest, forming a covalent adduct, a strategy that can present benefits over noncovalent inhibitors. This approach has gained much notoriety in recent years, mainly with diabetes and COVID-19-approved drugs. Nevertheless, the application of nitriles in covalent ligands is not restricted to it being the reactive center, as it can also be employed to convert irreversible inhibitors into reversible ones, a promising strategy for kinase inhibition and protein degradation. In this review, we introduce and discuss the roles of the cyano group in covalent inhibitors, how to tune its reactivity and the possibility of achieving selectivity only by replacing the warhead. Finally, we provide an overview of nitrile-based covalent compounds in approved drugs and inhibitors recently described in the literature.
Identifiers
What Socratic holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.