Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

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Abstract

Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase. © 2008 Elsevier Ltd. All rights reserved.

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Cee, V. J., Cheng, A. C., Romero, K., Bellon, S., Mohr, C., Whittington, D. A., … Geuns-Meyer, S. (2009). Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase. Bioorganic and Medicinal Chemistry Letters, 19(2), 424–427. https://doi.org/10.1016/j.bmcl.2008.11.056

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