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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

Authors :
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.
Source :
Bioorganic & Medicinal Chemistry Letters. Apr2006, Vol. 16 Issue 7, p1775-1779. 5p.
Publication Year :
2006

Abstract

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 EC50s<10nM. Ancillary hERG activity was evaluated for this series of inhibitors. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
16
Issue :
7
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
19842118
Full Text :
https://doi.org/10.1016/j.bmcl.2006.01.030