Abstract
Based on the lead compound BX-517, a series of C-4′ substituted indolinones have been synthesized and evaluated for PDK1 inhibition. Modification at C-4′ of the pyrrole afforded potent compounds (7b and 7d) with improved solubility and ADME properties. In this letter, we describe the synthesis, selectivity profile, and pharmacokinetic data of selected compounds. © 2007 Elsevier Ltd. All rights reserved.
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Islam, I., Brown, G., Bryant, J., Hrvatin, P., Kochanny, M. J., Phillips, G. B., … Arnaiz, D. O. (2007). Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: Optimization of BX-517. Bioorganic and Medicinal Chemistry Letters, 17(14), 3819–3825. https://doi.org/10.1016/j.bmcl.2007.05.060
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