2. Academic Validation
  3. Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP

Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP

  • Bioorg Med Chem Lett. 2006 Apr 1;16(7):1775-9. doi: 10.1016/j.bmcl.2006.01.030.
Mark E Fraley 1,  Robert M Garbaccio,  Kenneth L Arrington,  William F Hoffman,  Edward S Tasber,  Paul J Coleman,  Carolyn A Buser,  Eileen S Walsh,  Kelly Hamilton,  Christine Fernandes,  Michael D Schaber,  Robert B Lobell,  Weikang Tao,  Victoria J South,  Youwei Yan,  Lawrence C Kuo,  Thomayant Prueksaritanont,  Cathy Shu,  Maricel Torrent,  David C Heimbrook,  Nancy E Kohl,  Hans E Huber,  George D Hartman
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. mark_fraley@merck.com
PMID: 16439123 DOI: 10.1016/j.bmcl.2006.01.030
Abstract

The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780 human ovarian carcinoma cells with EC(50)s<10nM. Ancillary hERG activity was evaluated for this series of inhibitors.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-124790
    KSP抑制剂
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