7 research outputs found
The Use of Polymer‐Assisted Solution‐Phase Synthesis and Automation for the High‐Throughput Preparation of Biologically Active Compounds
No full textChromatography‐Free Suzuki Reactions Using a Polymer‐Assisted Solution‐Phase (PASP) Approach.
No full text
Chromatography-Free Suzuki Reactions Using a Polymer-Assisted Solution-Phase (PASP) Approach
No full textReporter Resins for Solid-Phase Chemistry
No full textAn analytical construct resin, designed to aid the analysis of solid-phase chemistry, has been mixed in a small proportion with a conventional
resin. The analytical construct (“reporter resin”) contains two orthogonal linkers that allow cleavage of either the synthetic intermediates (at
linker 2) or their analytically enhanced derivatives (at linker 1). The convenient and rapid monitoring of each step in the syntheses of representative
library compounds was possible using small resin aliquots
Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models
No full textAbstract
We describe here the identification and characterization of 2 novel inhibitors of the fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases. The compounds exhibit selective inhibition of FGFR over the closely related VEGFR2 receptor in cell lines and in vivo. The pharmacologic profile of these inhibitors was defined using a panel of human tumor cell lines characterized for specific mutations, amplifications, or translocations known to activate one of the four FGFR receptor isoforms. This pharmacology defines a profile for inhibitors that are likely to be of use in clinical settings in disease types where FGFR is shown to play an important role. Mol Cancer Ther; 10(9); 1542–52. ©2011 AACR.</jats:p
