ArticleBioorganic & medicinal chemistry letters2013
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 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
6 citing papers in PubMed.
- Exploring the Impact of Protein Chain Selection in Binding Energy Calculations with DFT.Chemphyschem : a European journal of chemical physics and physical chemistry · 2024Article
- Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy.Journal of hematology & oncology · 2018Review
- BEL Commons: an environment for exploration and analysis of networks encoded in Biological Expression Language.Database : the journal of biological databases and curation · 2018Article
- Dissecting fibrosis: therapeutic insights from the small-molecule toolbox.Nature reviews. Drug discovery · 2015Review
- Pharmacophore modeling of nilotinib as an inhibitor of ATP-binding cassette drug transporters and BCR-ABL kinase using a three-dimensional quantitative structure-activity relationship approach.Molecular pharmaceutics · 2014Article
- Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants.Cancer science · 2014Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
The importance of the trifluoromethyl group in the polypharmacological profile of nilotinib was investigated. Molecular editing of nilotinib led to the design, synthesis and biological evaluation of analogues where the trifluoromethyl group was replaced by a proton, fluorine and a methyl group. While these analogues were less active than nilotinib toward Abl, their activity toward Kit was comparable, with the monofluorinated analogue being the most active. Docking of nilotinib and of analogues 2a-c to the binding pocket of Abl and of Kit showed that the lack of shape complementarity in Kit is compensated by the stabilizing effect from its juxtamembrane region.
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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.