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Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

Farmer LJ, Bemis G, Britt SD, Cochran J, Connors M, Harrington EM, Hoock T, Markland W, Nanthakumar S, Taslimi P, Ter Haar E, Wang J, Zhaveri D, Salituro FG
Bioorg Med Chem Lett 18 6231-5 (2008)
Cited: 14 times
EuropePMC logo PMID: 18938080

Abstract

A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar K(i)'s against SYK and potent inhibition in mast cell degranulation assays.

Articles - 3emg mentioned but not cited (2)

  1. Predicting new indications for approved drugs using a proteochemometric method. Dakshanamurthy S, Issa NT, Assefnia S, Seshasayee A, Peters OJ, Madhavan S, Uren A, Brown ML, Byers SW. J Med Chem 55 6832-6848 (2012)
  2. A molecular mechanics approach to modeling protein-ligand interactions: relative binding affinities in congeneric series. Rapp C, Kalyanaraman C, Schiffmiller A, Schoenbrun EL, Jacobson MP. J Chem Inf Model 51 2082-2089 (2011)


Reviews citing this publication (4)

  1. Targeting innate immunity protein kinase signalling in inflammation. Gaestel M, Kotlyarov A, Kracht M. Nat Rev Drug Discov 8 480-499 (2009)
  2. Spleen tyrosine kinases: biology, therapeutic targets and drugs. Riccaboni M, Bianchi I, Petrillo P. Drug Discov Today 15 517-530 (2010)
  3. Inhibitors of switch kinase 'spleen tyrosine kinase' in inflammation and immune-mediated disorders: a review. Kaur M, Singh M, Silakari O. Eur J Med Chem 67 434-446 (2013)
  4. Therapeutic prospect of Syk inhibitors. Ruzza P, Biondi B, Calderan A. Expert Opin Ther Pat 19 1361-1376 (2009)

Articles citing this publication (8)

  1. Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics. Zhao H, Caflisch A. Bioorg Med Chem Lett 23 5721-5726 (2013)
  2. Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors. Xie HZ, Li LL, Ren JX, Zou J, Yang L, Wei YQ, Yang SY. Bioorg Med Chem Lett 19 1944-1949 (2009)
  3. Discovery of new Syk inhibitors through structure-based virtual screening. Huang Y, Zhang Y, Fan K, Dong G, Li B, Zhang W, Li J, Sheng C. Bioorg Med Chem Lett 27 1776-1779 (2017)
  4. In silico prediction of spleen tyrosine kinase inhibitors using machine learning approaches and an optimized molecular descriptor subset generated by recursive feature elimination method. Li BK, Cong Y, Yang XG, Xue Y, Chen YZ. Comput Biol Med 43 395-404 (2013)
  5. Discovery of a Potent Candidate for RET-Specific Non-Small-Cell Lung Cancer-A Combined In Silico and In Vitro Strategy. Ramesh P, Shin WH, Veerappapillai S. Pharmaceutics 13 1775 (2021)
  6. Application of cultured human mast cells (CHMC) for the design and structure-activity relationship of IgE-mediated mast cell activation inhibitors. Argade A, Bhamidipati S, Li H, Carroll D, Clough J, Keim H, Sylvain C, Rossi AB, Coquilla C, Issakani SD, Masuda ES, Payan DG, Singh R. Bioorg Med Chem Lett 25 2117-2121 (2015)
  7. Applying ligands profiling using multiple extended electron distribution based field templates and feature trees similarity searching in the discovery of new generation of urea-based antineoplastic kinase inhibitors. Dokla EM, Mahmoud AH, Elsayed MS, El-Khatib AH, Linscheid MW, Abouzid KA. PLoS One 7 e49284 (2012)
  8. 3D-QSAR-Based Pharmacophore Modeling, Virtual Screening, and Molecular Dynamics Simulations for the Identification of Spleen Tyrosine Kinase Inhibitors. Kumar V, Parate S, Danishuddin, Zeb A, Singh P, Lee G, Jung TS, Lee KW, Ha MW. Front Cell Infect Microbiol 12 909111 (2022)


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