| Literature DB >> 17761419 |
Paul J Coleman1, John D Schreier, Christopher D Cox, Mark E Fraley, Robert M Garbaccio, Carolyn A Buser, Eileen S Walsh, Kelly Hamilton, Robert B Lobell, Keith Rickert, Weikang Tao, Ronald E Diehl, Vicki J South, Joseph P Davide, Nancy E Kohl, Youwei Yan, Lawrence Kuo, Thomayant Prueksaritanont, Chunze Li, Elizabeth A Mahan, Carmen Fernandez-Metzler, Joseph J Salata, George D Hartman.
Abstract
3,5-diaryl-4,5-dihydropyrazoles were discovered to be potent KSP inhibitors with excellent in vivo potency. These enzyme inhibitors possess desirable physical properties that can be readily modified by incorporation of a weakly basic amine. Careful adjustment of amine basicity was essential for preserving cellular potency in a multidrug resistant cell line while maintaining good aqueous solubility.Entities:
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Year: 2007 PMID： 17761419 DOI： 10.1016/j.bmcl.2007.07.046
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823