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Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.

Authors :
Roecker AJ
Coleman PJ
Mercer SP
Schreier JD
Buser CA
Walsh ES
Hamilton K
Lobell RB
Tao W
Diehl RE
South VJ
Davide JP
Kohl NE
Yan Y
Kuo LC
Li C
Fernandez-Metzler C
Mahan EA
Prueksaritanont T
Hartman GD
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Oct 15; Vol. 17 (20), pp. 5677-82. Date of Electronic Publication: 2007 Aug 21.
Publication Year :
2007

Abstract

Inspired by previous efforts in the pyrazolobenzoxazine class of KSP inhibitors, the design and synthesis of 1,4-diaryl-4,5-dihydropyrazole inhibitors of KSP are described. Crystallographic evidence of binding mode and in vivo potency data is also highlighted.

Details

Language :
English
ISSN :
0960-894X
Volume :
17
Issue :
20
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
17766111
Full Text :
https://doi.org/10.1016/j.bmcl.2007.07.074