| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373451 | Bioorganic & Medicinal Chemistry Letters | 2007 | 7 Pages |
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.
Graphical abstractOptimization of BX-517 afforded 7b, an inhibitor of PDK1 with improved physicochemical properties.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Imadul Islam, Greg Brown, Judi Bryant, Paul Hrvatin, Monica J. Kochanny, Gary B. Phillips, Shendong Yuan, Marc Adler, Marc Whitlow, Dao Lentz, Mark A. Polokoff, James Wu, Jun Shen, Janette Walters, Elena Ho, Babu Subramanyam, Daguang Zhu,