Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517

  • Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25. doi: 10.1016/j.bmcl.2007.05.060.
Imadul Islam  1 ,  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 ,  Richard I Feldman ,  Damian O Arnaiz
Affiliations
PMID: 17544272 DOI: 10.1016/j.bmcl.2007.05.060
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.

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