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Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517 |
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| Authors: | Islam Imadul Brown Greg Bryant Judi Hrvatin Paul Kochanny Monica J Phillips Gary B Yuan Shendong Adler Marc Whitlow Marc Lentz Dao Polokoff Mark A Wu James Shen Jun Walters Janette Ho Elena Subramanyam Babu Zhu Daguang Feldman Richard I Arnaiz Damian O |
| Institution: | Berlex Biosciences, 2600 Hilltop Dr. Richmond, CA 94804, USA. imadulislam@yahoo.com |
| 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. |
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