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
|
Тип публикации: Journal Article
Дата публикации: 2007-10-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
17766111
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
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.
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Roecker A. et al. 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 // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 20. pp. 5677-5682.
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Roecker A., Coleman P., Mercer S. P., Schreier J. D., Buser C. A., Walsh E. S., Hamilton K., Lobell R. B., Tao W., Diehl R. E., South V. J., Davide J. P., Kohl N. E., Yan Y., Kuo L. C., Li C., Fernandez-Metzler C., Mahan E. A., Prueksaritanont T., Hartman G. W. 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 // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 20. pp. 5677-5682.
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TY - JOUR
DO - 10.1016/j.bmcl.2007.07.074
UR - https://doi.org/10.1016/j.bmcl.2007.07.074
TI - 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
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Roecker, A.J.
AU - Coleman, Paul
AU - Mercer, Swati P
AU - Schreier, John D
AU - Buser, Carolyn A.
AU - Walsh, Eileen S.
AU - Hamilton, Kelly
AU - Lobell, Robert B.
AU - Tao, Weikang
AU - Diehl, Ronald E.
AU - South, Vicki J
AU - Davide, Joseph P
AU - Kohl, Nancy E.
AU - Yan, Youwei
AU - Kuo, Lawrence C.
AU - Li, Chunze
AU - Fernandez-Metzler, Carmen
AU - Mahan, Elizabeth A
AU - Prueksaritanont, Thomayant
AU - Hartman, George W.
PY - 2007
DA - 2007/10/01
PB - Elsevier
SP - 5677-5682
IS - 20
VL - 17
PMID - 17766111
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2007_Roecker,
author = {A.J. Roecker and Paul Coleman and Swati P Mercer and John D Schreier and Carolyn A. Buser and Eileen S. Walsh and Kelly Hamilton and Robert B. Lobell and Weikang Tao and Ronald E. Diehl and Vicki J South and Joseph P Davide and Nancy E. Kohl and Youwei Yan and Lawrence C. Kuo and Chunze Li and Carmen Fernandez-Metzler and Elizabeth A Mahan and Thomayant Prueksaritanont and George W. Hartman},
title = {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},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2007},
volume = {17},
publisher = {Elsevier},
month = {oct},
url = {https://doi.org/10.1016/j.bmcl.2007.07.074},
number = {20},
pages = {5677--5682},
doi = {10.1016/j.bmcl.2007.07.074}
}
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MLA
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Roecker, A.J., et al. “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.” Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 20, Oct. 2007, pp. 5677-5682. https://doi.org/10.1016/j.bmcl.2007.07.074.