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Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.

Bardelle C, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ
Bioorg Med Chem Lett 18 2776-80 (2008)
Related entries: 2vwu, 2vwv, 2vx0

Cited: 32 times
EuropePMC logo PMID: 18434142

Abstract

A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.

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  1. Eph receptors and ephrins in cancer: bidirectional signalling and beyond. Pasquale EB. Nat Rev Cancer 10 165-180 (2010)
  2. Therapeutic targeting of EPH receptors and their ligands. Boyd AW, Bartlett PF, Lackmann M. Nat Rev Drug Discov 13 39-62 (2014)
  3. Targeting Eph receptors with peptides and small molecules: progress and challenges. Noberini R, Lamberto I, Pasquale EB. Semin Cell Dev Biol 23 51-57 (2012)
  4. EphB4: A promising target for upper aerodigestive malignancies. Salgia R, Kulkarni P, Gill PS. Biochim Biophys Acta Rev Cancer 1869 128-137 (2018)
  5. The critical role of the interplays of EphrinB2/EphB4 and VEGF in the induction of angiogenesis. Du E, Li X, He S, Li X, He S. Mol Biol Rep 47 4681-4690 (2020)
  6. New strategies in achieving antiangiogenic effect: Multiplex inhibitors suppressing compensatory activations of RTKs. Shan Y, Wang B, Zhang J. Med Res Rev 38 1674-1705 (2018)
  7. The status of isocyanide-based multi-component reactions in Iran (2010-2018). Shaabani A, Mohammadian R, Afshari R, Hooshmand SE, Nazeri MT, Javanbakht S. Mol Divers 25 1145-1210 (2021)

Articles citing this publication (23)

  1. The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis. Martiny-Baron G, Holzer P, Billy E, Schnell C, Brueggen J, Ferretti M, Schmiedeberg N, Wood JM, Furet P, Imbach P. Angiogenesis 13 259-267 (2010)
  2. Kinase selectivity potential for inhibitors targeting the ATP binding site: a network analysis. Huang D, Zhou T, Lafleur K, Nevado C, Caflisch A. Bioinformatics 26 198-204 (2010)
  3. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Choi Y, Syeda F, Walker JR, Finerty PJ, Cuerrier D, Wojciechowski A, Liu Q, Dhe-Paganon S, Gray NS. Bioorg Med Chem Lett 19 4467-4470 (2009)
  4. Eph receptors and ephrin ligands: important players in angiogenesis and tumor angiogenesis. Mosch B, Reissenweber B, Neuber C, Pietzsch J. J Oncol 2010 135285 (2010)
  5. The EphB4 receptor tyrosine kinase promotes lung cancer growth: a potential novel therapeutic target. Ferguson BD, Liu R, Rolle CE, Tan YH, Krasnoperov V, Kanteti R, Tretiakova MS, Cervantes GM, Hasina R, Hseu RD, Iafrate AJ, Karrison T, Ferguson MK, Husain AN, Faoro L, Vokes EE, Gill PS, Salgia R. PLoS One 8 e67668 (2013)
  6. Hydrogen bonding penalty upon ligand binding. Zhao H, Huang D. PLoS One 6 e19923 (2011)
  7. Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines. Bardelle C, Coleman T, Cross D, Davenport S, Kettle JG, Ko EJ, Leach AG, Mortlock A, Read J, Roberts NJ, Robins P, Williams EJ. Bioorg Med Chem Lett 18 5717-5721 (2008)
  8. Dispensing processes impact apparent biological activity as determined by computational and statistical analyses. Ekins S, Olechno J, Williams AJ. PLoS One 8 e62325 (2013)
  9. Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series. Barlaam B, Ducray R, Lambert-van der Brempt C, Plé P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J. Bioorg Med Chem Lett 21 2207-2211 (2011)
  10. Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics. Zhao H, Dong J, Lafleur K, Nevado C, Caflisch A. ACS Med Chem Lett 3 834-838 (2012)
  11. Fluorine-18 radiolabeling and radiopharmacological characterization of a benzodioxolylpyrimidine-based radiotracer targeting the receptor tyrosine kinase EphB4. Mamat C, Mosch B, Neuber C, Köckerling M, Bergmann R, Pietzsch J. ChemMedChem 7 1991-2003 (2012)
  12. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Qiao L, Choi S, Case A, Gainer TG, Seyb K, Glicksman MA, Lo DC, Stein RL, Cuny GD. Bioorg Med Chem Lett 19 6122-6126 (2009)
  13. A novel benzodioxole-containing inhibitor of Toxoplasma gondii growth alters the parasite cell cycle. Kamau E, Meehan T, Lavine MD, Arrizabalaga G, Mustata Wilson G, Boyle J. Antimicrob Agents Chemother 55 5438-5451 (2011)
  14. Completing the structural family portrait of the human EphB tyrosine kinase domains. Overman RC, Debreczeni JE, Truman CM, McAlister MS, Attwood TK. Protein Sci 23 627-638 (2014)
  15. Modeling error in experimental assays using the bootstrap principle: understanding discrepancies between assays using different dispensing technologies. Hanson SM, Ekins S, Chodera JD. J Comput Aided Mol Des 29 1073-1086 (2015)
  16. Biochemical and biophysical characterization of four EphB kinase domains reveals contrasting thermodynamic, kinetic and inhibition profiles. Overman RC, Debreczeni JE, Truman CM, McAlister MS, Attwood TK. Biosci Rep 33 e00040 (2013)
  17. Preparation of a novel radiotracer targeting the EphB4 receptor via radiofluorination using spiro azetidinium salts as precursor. Wiemer J, Steinbach J, Pietzsch J, Mamat C. J Labelled Comp Radiopharm 60 489-498 (2017)
  18. EphB4 cellular kinase activity assayed using an enzymatic protein interaction system. Wehrman T, Nguyen M, Feng W, Bader B. Assay Drug Dev Technol 11 237-243 (2013)
  19. Stability and solubility engineering of the EphB4 tyrosine kinase catalytic domain using a rationally designed synthetic library. Overman RC, Green I, Truman CM, Read JA, Embrey KJ, McAlister MS, Attwood TK. Protein Eng Des Sel 26 695-704 (2013)
  20. An investigation of binding interactions of tumor-targeted peptide conjugated polyphenols with the kinase domain of ephrin B4 and B2 receptors. Mitchell SM, Heise RM, Murray ME, Lambo DJ, Daso RE, Banerjee IA. Mol Divers (2023)
  21. Identifying potential selective fluorescent probes for cancer-associated protein carbonic anhydrase IX using a computational approach. Kamstra RL, Floriano WB. J Mol Graph Model 54 184-193 (2014)
  22. N-(2,4)-dinitrophenyl-L-arginine Interacts with EphB4 and Functions as an EphB4 Kinase Modulator. Kamstra RL, Freywald A, Floriano WB. Chem Biol Drug Des 86 476-486 (2015)
  23. Styrylquinazoline derivatives as ABL inhibitors selective for different DFG orientations. Malarz K, Mularski J, Pacholczyk M, Musiol R. J Enzyme Inhib Med Chem 38 2201410 (2023)


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