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

Imadul Islam Judi Bryant Yuo-Ling Chou Monica J Kochanny Wheeseong Lee Gary B Phillips Hongyi Yu Marc Adler Marc Whitlow Elena Ho Dao Lentz Mark A Polokoff Babu Subramanyam James M Wu Daguang Zhu Richard I Feldman Damian O Arnaiz

Bioorg Med Chem Lett

Berlex Biosciences, 2600 Hilltop Dr. Richmond, CA 94804, USA.

Published: July 2007

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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 Source
http://dx.doi.org/10.1016/j.bmcl.2007.04.071DOI Listing

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