Evidence map›Paper›PMID 28181424›Full record

ArticleChemMedChem2017

Medicinal Chemistry Profiling of Monocyclic 1,2-Azaborines.

Peng Zhao, David O Nettleton, Rajeshri G Karki, Frédéric J Zécri, Shih-Yuan Liu

Abstract read
In one paragraph

Article in ChemMedChem, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.

0numbers the graph read from it
0cells of the map it votes in
39citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

39 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
  4. A Catalyst-Controlled Divergent Rearomatization of BN-Benzvalene.Journal of the American Chemical Society · 2026
    Article
  5. Article
  6. Positional Isomerization of 1,2-Azaborine through BN-Benzvalene.Journal of the American Chemical Society · 2026
    Article
  7. Article
  8. Article
  9. Review
  10. Review
  11. Article
  12. Article
  13. Boron-Nitrogen-Containing Benzene Valence Isomers.Chemistry (Weinheim an der Bergstrasse, Germany) · 2024
    Article
  14. Article
  15. Article
  16. Synthesis and crystal structure of bis-(9-mesityl-9,10-di-hydro-10-aza-9-borabenzo[Acta crystallographica. Section E, Crystallographic communications · 2023
    Article
  17. Article
  18. The aromatic Claisen rearrangement of a 1,2-azaborine.Organic & biomolecular chemistry · 2023
    Article
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors.

Peng ZhaoDepartment of Chemistry, Boston College, Chestnut Hill, MA, 02467, USA.
David O NettletonNovartis Institutes for Biomedical Research, 181 Massachusetts Avenue, Cambridge, MA, 02139, USA.
Rajeshri G KarkiNovartis Institutes for Biomedical Research, 181 Massachusetts Avenue, Cambridge, MA, 02139, USA.
Frédéric J ZécriNovartis Institutes for Biomedical Research, 181 Massachusetts Avenue, Cambridge, MA, 02139, USA.
Shih-Yuan LiuDepartment of Chemistry, Boston College, Chestnut Hill, MA, 02467, USA.

Funding

Development of BN Heterocycles for Biomedical ResearchR01GM094541 · NIGMS · UNIVERSITY OF OREGON · PI LIU, SHIH-YUAN · 2010 to 2019
$2.8M
NIGMS NIH HHS R01 GM094541
6 · The paper itself

Abstract

The first examples of biologically active monocyclic 1,2-azaborines have been synthesized and demonstrated to exhibit not only improved in vitro aqueous solubility in comparison with their corresponding carbonaceous analogues, but in the context of a CDK2 inhibitor, also improved biological activity and better in vivo oral bioavailability. This proof-of-concept study establishes the viability of monocyclic 1,2-azaborines as a novel pharmacophore with distinct pharmacological profiles that can help address challenges associated with solubility in drug development research.

Indexed as

Administration, OralAnimalsBinding SitesBoron CompoundsChemistry, PharmaceuticalCyclin-Dependent Kinase 2Half-LifeHydrogen BondingMaleMolecular Dynamics SimulationProtein Kinase InhibitorsProtein Structure, TertiaryRatsRats, Sprague-DawleySolubility1,2-azaborineBoron CompoundsCyclin-Dependent Kinase 2Protein Kinase InhibitorsazaborinesBN heterocycleCDK2 inhibitorsdrug discoverysolubility

Identifiers

PMID28181424
PMCPMC5654323

What OpenQuestion holds

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Registered trials

None linked

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.