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Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.

Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E
Bioorg Med Chem Lett 18 5115-7 (2008)
Cited: 2 times
EuropePMC logo PMID: 18723346

Abstract

Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors has been shown clinically to successfully treat gastrointestinal stromal tumors and mastocytosis. Targeted therapy of c-Kit activity may provide therapeutic advantages against off-target effects for non-oncology applications. A new structural class of c-Kit inhibitors is described, including in vitro c-Kit potency, kinase selectivity, and the observed binding mode.

Articles citing this publication (2)

  1. Receptor-guided 3D-QSAR approach for the discovery of c-kit tyrosine kinase inhibitors. Almerico AM, Tutone M, Lauria A. J Mol Model 18 2885-2895 (2012)
  2. Phenolate-Induced N-O Bond Formation versus TiemannType Rearrangement for the Synthesis of 3-Aminobenzisoxazoles and 2-Aminobenzoxazoles. Hufnagel B, Zhu WF, Franz HM, Proschak E, Hernandez-Olmos V. ChemistryOpen 11 e202200252 (2022)


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