3kf7 › Citations

Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition.

Jerome KD, Rucker PV, Xing L, Shieh HS, Baldus JE, Selness SR, Letavic MA, Braganza JF, McClure KF
Bioorg Med Chem Lett 20 469-73 (2010)
Cited: 7 times
EuropePMC logo PMID: 19969459

Abstract

The structure based drug design, synthesis and structure-activity relationship of a series of C6 sulfur linked triazolopyridine based p38 inhibitors are described. The metabolic deficiencies of this series were overcome through changes in the C6 linker from sulfur to methylene, which was predicted by molecular modeling to be bioisosteric. X-ray of the ethylene linked compound 61 confirmed the predicted binding orientation of the scaffold in the p38 enzyme.

Articles - 3kf7 mentioned but not cited (3)

  1. Identification of gefitinib off-targets using a structure-based systems biology approach; their validation with reverse docking and retrospective data mining. Verma N, Rai AK, Kaushik V, Brünnert D, Chahar KR, Pandey J, Goyal P. Sci Rep 6 33949 (2016)
  2. Network Pharmacology and Bioinformatics Methods Reveal the Mechanism of Berberine in the Treatment of Ischaemic Stroke. Song K, Sun Y, Liu H, Li Y, An N, Wang L, Zhang H, Yang F, Xing Y, Gao Y. Evid Based Complement Alternat Med 2022 5160329 (2022)
  3. p38α Mitogen-Activated Protein Kinase Is a Druggable Target in Pancreatic Adenocarcinoma. Yang L, Sun X, Ye Y, Lu Y, Zuo J, Liu W, Elcock A, Zhu S. Front Oncol 9 1294 (2019)


Reviews citing this publication (2)

  1. p38α mitogen-activated protein kinase inhibitors, a patent review (2005-2011). Fischer S, Koeberle SC, Laufer SA. Expert Opin Ther Pat 21 1843-1866 (2011)
  2. A Comprehensive Structural Overview of p38α MAPK in Complex with Type I Inhibitors. Astolfi A, Iraci N, Manfroni G, Barreca ML, Cecchetti V. ChemMedChem 10 957-969 (2015)

Articles citing this publication (2)

  1. Development of Novel In Vivo Chemical Probes to Address CNS Protein Kinase Involvement in Synaptic Dysfunction. Watterson DM, Grum-Tokars VL, Roy SM, Schavocky JP, Bradaric BD, Bachstetter AD, Xing B, Dimayuga E, Saeed F, Zhang H, Staniszewski A, Pelletier JC, Minasov G, Anderson WF, Arancio O, Van Eldik LJ. PLoS ONE 8 e66226 (2013)
  2. Virtual screening using a conformationally flexible target protein: models for ligand binding to p38α MAPK. Vinh NB, Simpson JS, Scammells PJ, Chalmers DK. J. Comput. Aided Mol. Des. 26 409-423 (2012)


Quick links