ReviewChemistry & biology2014
Privileged diazepine compounds and their emergence as bromodomain inhibitors.
Review in Chemistry & biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
23 citing papers in PubMed, 78 citations in OpenAlex.
- Recent advances in synthesis and medicinal chemistry of pyrrolodiazepines.Frontiers in chemistry · 2026Review
- Novel 1,4-Diazepane derivatives as amyloid-beta (Aβ) aggregation inhibitors.Frontiers in chemistry · 2026Article
- Design, synthesis, and bioevaluation of pyrazole-containing tubulin polymerisation inhibitors based on conformational constraint strategy.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- In Silico and in vitro evaluation of the anticancer effect of a 1,5-Benzodiazepin-2-One derivative (3b) revealing potent dual inhibition of HER2 and HDAC1.Scientific reports · 2025Article
- Targeting lysine acetylation readers and writers.Nature reviews. Drug discovery · 2025Review
- The shikimate pathway: gateway to metabolic diversity.Natural product reports · 2024Review
- Bromodomain inhibitors and therapeutic applications.Current opinion in chemical biology · 2023Review
- The anti-Alzheimer potential of novel spiroindolin-1,2-diazepine derivatives as targeted cholinesterase inhibitors with modified substituents.Scientific reports · 2023Article
- Streamlined DNA-encoded small molecule library screening and validation for the discovery of novel chemotypes targeting BET proteins.Molecular therapy. Nucleic acids · 2023Article
- Synthesis and Structure-Activity Relationships of Aristoyagonine Derivatives as Brd4 Bromodomain Inhibitors with X-ray Co-Crystal Research.Molecules (Basel, Switzerland) · 2021Article
- Bromodomain biology and drug discovery.Nature structural & molecular biology · 2019Review
- Diverse Isoquinoline Scaffolds by Ugi/Pomeranz-Fritsch and Ugi/Schlittler-Müller Reactions.Organic letters · 2019Article
- Molecules targeting the androgen receptor (AR) signaling axis beyond the AR-Ligand binding domain.Medicinal research reviews · 2019Review
- Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.Journal of medicinal chemistry · 2018Article
- Targeting Cancer Cells with BET Bromodomain Inhibitors.Cold Spring Harbor perspectives in medicine · 2017Review
- Diversity-oriented synthetic strategy for developing a chemical modulator of protein-protein interaction.Nature communications · 2016Article
- Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology.Future medicinal chemistry · 2016Review
- Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7.ACS medicinal chemistry letters · 2016Article
- Small Molecule Inhibitor of CBFβ-RUNX Binding for RUNX Transcription Factor Driven Cancers.EBioMedicine · 2016Article
- The Bromodomain: A New Target in Emerging Epigenetic Medicine.ACS chemical biology · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Chemical compounds built on a diazepine scaffold have recently emerged as potent inhibitors of the acetyl-lysine binding activity of bromodomain-containing proteins, which is required for gene transcriptional activation in cancer and inflammation. Not only have these chemical compounds validated bromodomains as attractive epigenetic drug targets, but they have also brought to the forefront another application of the diazepine, which had already been regarded as a versatile chemical scaffold in rational drug design. This article reviews the success of diazepine compounds as therapeutic agents and examines the unique chemical and geometric features of this privileged scaffold that make it an excellent template for developing potent and selective molecules that control bromodomain-related gene expression in human diseases.
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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 OpenQuestion graph.