Details

Autor(en) / Beteiligte

• Fraley, Mark E.
• Garbaccio, Robert M.
• Arrington, Kenneth L.
• Hoffman, William F.
• Tasber, Edward S.
• Coleman, Paul J.
• Buser, Carolyn A.
• Walsh, Eileen S.
• Hamilton, Kelly
• Fernandes, Christine
• Schaber, Michael D.
• Lobell, Robert B.
• Tao, Weikang
• South, Victoria J.
• Yan, Youwei
• Kuo, Lawrence C.
• Prueksaritanont, Thomayant
• Shu, Cathy
• Torrent, Maricel
• Heimbrook, David C.
• Kohl, Nancy E.
• Huber, Hans E.
• Hartman, George D.

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (7), p.1775-1779

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2006

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 2,4-Diaryl-2,5-dihydropyrroles are reported as potent inhibitors of the mitotic kinesin KSP. 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 50s < 10 nM. Ancillary hERG activity was evaluated for this series of inhibitors.