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Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity |
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| Authors: | Islam Imadul Bryant Judi Chou Yuo-Ling Kochanny Monica J Lee Wheeseong Phillips Gary B Yu Hongyi Adler Marc Whitlow Marc Ho Elena Lentz Dao Polokoff Mark A Subramanyam Babu Wu James M Zhu Daguang Feldman Richard I Arnaiz Damian O |
| Institution: | Berlex Biosciences, 2600 Hilltop Dr. Richmond, CA 94804, USA. |
| 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. |
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| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |