Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: Design, synthesis and biological activity

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Abstract

HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA. © 2007 Elsevier Ltd. All rights reserved.

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Islam, I., Bryant, J., Chou, Y. L., Kochanny, M. J., Lee, W., Phillips, G. B., … Arnaiz, D. O. (2007). Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: Design, synthesis and biological activity. Bioorganic and Medicinal Chemistry Letters, 17(14), 3814–3818. https://doi.org/10.1016/j.bmcl.2007.04.071

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