639074-95-6Relevant articles and documents
Kinesin spindle protein (KSP) inhibitors. Part 3: Synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility
Garbaccio, Robert M.,Fraley, Mark E.,Tasber, Edward S.,Olson, Christy M.,Hoffman, William F.,Arrington, Kenneth L.,Torrent, Maricel,Buser, Carolyn A.,Walsh, Eileen S.,Hamilton, Kelly,Schaber, Michael D.,Fernandes, Christine,Lobell, Robert B.,Tao, Weikang,South, Vicki J.,Yan, Youwei,Kuo, Lawrence C.,Prueksaritanont, Thomayant,Slaughter, Donald E.,Shu, Cathy,Heimbrook, David C.,Kohl, Nancy E.,Huber, Hans E.,Hartman, George D.
, p. 1780 - 1783 (2007/10/03)
2,4-Diaryl-2,5-dihydropyrroles have been discovered to be novel, potent and water-soluble inhibitors of KSP, an emerging therapeutic target for the treatment of cancer. A potential concern for these basic KSP inhibitors (1 and 2) was hERG binding that can be minimized by incorporation of a potency-enhancing C2 phenol combined with neutral N1 side chains. Aqueous solubility was restored to these, and other, non-basic inhibitors, through a phosphate prodrug strategy.
