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

  • Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. doi: 10.1016/j.bmcl.2007.04.071.
Imadul Islam  1 ,  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
Affiliations
  • 1. Berlex Biosciences, 2600 Hilltop Dr. Richmond, CA 94804, USA.
PMID: 17531483 DOI: 10.1016/j.bmcl.2007.04.071
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.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13842
    BX517
    98.0%, PDK-1 Inhibitor
    target: PDK-1
    Research Areas: Cancer