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

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

Affiliation

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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13842
    ≥98.0%, PDK-1 Inhibitor