Bioorganic and Medicinal Chemistry Letters, volume 17, issue 20, pages 5677-5682
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
A.J. Roecker
1
,
Paul Coleman
1
,
Swati P Mercer
1
,
John D Schreier
1
,
Carolyn A. Buser
2
,
Eileen S. Walsh
2
,
Kelly Hamilton
2
,
Robert B. Lobell
2
,
Weikang Tao
2
,
Ronald E. Diehl
2
,
Vicki J South
2
,
Joseph P Davide
2
,
Nancy E. Kohl
2
,
Youwei Yan
3
,
Lawrence C. Kuo
3
,
Chunze Li
4
,
Carmen Fernandez-Metzler
4
,
Elizabeth A Mahan
4
,
Thomayant Prueksaritanont
4
,
George W. Hartman
1
1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA.
|
2
Department of Cancer Research, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
|
3
Department of Structural Biology, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
|
4
Department of Drug Metabolism, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
|
Publication type: Journal Article
Publication date: 2007-10-01
scimago Q2
wos Q2
SJR: 0.508
CiteScore: 5.7
Impact factor: 2.5
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
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.
Found
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.