946847-38-7Relevant articles and documents
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: Optimization of BX-517
Islam, Imadul,Brown, Greg,Bryant, Judi,Hrvatin, Paul,Kochanny, Monica J.,Phillips, Gary B.,Yuan, Shendong,Adler, Marc,Whitlow, Marc,Lentz, Dao,Polokoff, Mark A.,Wu, James,Shen, Jun,Walters, Janette,Ho, Elena,Subramanyam, Babu,Zhu, Daguang,Feldman, Richard I.,Arnaiz, Damian O.
, p. 3819 - 3825 (2008/02/07)
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.
