ArticleThe Journal of organic chemistry2014
Emission tuning of fluorescent kinase inhibitors: conjugation length and substituent effects.
Article in The Journal of organic chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 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
11 citing papers in PubMed, 32 citations in OpenAlex.
- Novel EGFR tyrosine kinase inhibitors exhibiting intrinsic fluorescence.Investigational new drugs · 2026Article
- Design Principles and Applications of Fluorescent Kinase Inhibitors for Simultaneous Cancer Bioimaging and Therapy.Cancers · 2024Review
- A dual inhibitor of PIP5K1C and PIKfyve prevents SARS-CoV-2 entry into cells.Experimental & molecular medicine · 2024Article
- Intrinsically Fluorescent Anti-Cancer Drugs.Biology · 2022Review
- Quinazoline Based HDAC Dual Inhibitors as Potential Anti-Cancer Agents.Molecules (Basel, Switzerland) · 2022Review
- Fluorescent kinase inhibitors as probes in cancer.Chemical Society reviews · 2021Review
- A Fluorescent Kinase Inhibitor that Exhibits Diagnostic Changes in Emission upon Binding.Angewandte Chemie (International ed. in English) · 2019Article
- Synthesis and In Vitro Cytotoxic Properties of Polycarbo-Substituted 4-(Arylamino)quinazolines.Molecules (Basel, Switzerland) · 2016Article
- Binding-induced, turn-on fluorescence of the EGFR/ERBB kinase inhibitor, lapatinib.Organic & biomolecular chemistry · 2015Article
- Advances in metal-catalyzed cross-coupling reactions of halogenated quinazolinones and their quinazoline derivatives.Molecules (Basel, Switzerland) · 2014Review
- Visibly emissive and responsive extended 6-aza-uridines.Organic letters · 2014Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Fluorescent N-phenyl-4-aminoquinazoline probes targeting the ATP-binding pocket of the ERBB family of receptor tyrosine kinases are reported. Extension of the aromatic quinazoline core with fluorophore "arms" through substitution at the 6- position of the quinazoline core with phenyl, styryl, and phenylbutadienyl moieties was predicted by means of TD-DFT calculations to produce probes with tunable photoexcitation energies and excited states possessing charge-transfer character. Optical spectroscopy identified several synthesized probes that are nonemissive in aqueous solutions and exhibit emission enhancements in solvents of low polarity, suggesting good performance as turn-on fluorophores. Ligand-induced ERBB2 phosphorylation assays demonstrate that despite chemical modification to the quinazoline core these probes still function as ERBB2 inhibitors in MCF7 cells. Two probes were found to exhibit ERBB2-induced fluorescence, demonstrating the utility of these probes as turn-on, fluoroescent kinase inhibitors.
Indexed as
Identifiers
What OpenQuestion 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 OpenQuestion graph.