ArticleBioorganic & medicinal chemistry letters2009
Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.
Article in Bioorganic & medicinal chemistry letters, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 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.
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Who cites it
12 citing papers in PubMed, 29 citations in OpenAlex.
- Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.Journal of medicinal chemistry · 2024Article
- Identification of potent pan-ephrin receptor kinase inhibitors using DNA-encoded chemistry technology.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Eph Receptors in Cancer.Biomedicines · 2023Review
- Hit Identification of a Novel Quinazoline Sulfonamide as a Promising EphB3 Inhibitor: Design, Virtual Combinatorial Library, Synthesis, Biological Evaluation, and Docking Simulation Studies.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Barcoded viral tracing of single-cell interactions in central nervous system inflammation.Science (New York, N.Y.) · 2021Article
- Transcriptional Dependencies in Diffuse Intrinsic Pontine Glioma.Cancer cell · 2017Article
- Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3.Journal of the American Chemical Society · 2016Article
- Completing the structural family portrait of the human EphB tyrosine kinase domains.Protein science : a publication of the Protein Society · 2014Article
- Biochemical and biophysical characterization of four EphB kinase domains reveals contrasting thermodynamic, kinetic and inhibition profiles.Bioscience reports · 2013Article
- Eph receptors and ephrins as targets for cancer therapy.Journal of cellular and molecular medicine · 2012Review
- Targeting Eph receptors with peptides and small molecules: progress and challenges.Seminars in cell & developmental biology · 2012Review
- Eph receptors and ephrins in cancer: bidirectional signalling and beyond.Nature reviews. Cancer · 2010Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a phenyl or small electron donating substituents to the 5-position of the pyrazolo[1,5-a]pyridine. In addition, replacement of the pyrazolo[1,5-a]pyridine with imidazo[1,2-a]pyridine was well tolerated and resulted in enhanced mouse liver microsome stability. The structure-activity relationship for EphB3 inhibition of both heterocyclic series was similar. Kinase inhibitory activity was also demonstrated for representative analogs in cell culture. An analog (32, LDN-211904) was also profiled for inhibitory activity against a panel of 288 kinases and found to be quite selective for tyrosine kinases. Overall, these studies provide useful molecular probes for examining the in vitro, cellular and potentially in vivo kinase-dependent function of EphB3 receptor.
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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.