Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors

Matthew R. Kaller; Wenge Zhong; Charles Henley; Ella Magal; Thomas Nguyen; David Powers; Robert M. Rzasa; Weiya Wang; Xiaoling Xiong; Mark H. Norman

doi:10.1016/j.bmcl.2009.10.027

Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors

Matthew R. Kaller
, Wenge Zhong
, Charles Henley
, Ella Magal
, Thomas Nguyen
, David Powers
, Robert M. Rzasa
, Weiya Wang
, Xiaoling Xiong
, Mark H. Norman

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

Abstract

Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved in neurodegenerative disorders. Using active site homology and previous structure-activity relationships, a new series of potent CDK5 inhibitors was designed. This report describes the optimization of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.

Original language	English
Pages (from-to)	6591-6594
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2009.10.027
State	Published - 1 Dec 2009
Externally published	Yes

Keywords

6-Oxo-1,6-dihydropyridines
CDK5 inhibitor
Kinase
Neurodegenerative disorders

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10.1016/j.bmcl.2009.10.027

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title = "Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors",

abstract = "Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved in neurodegenerative disorders. Using active site homology and previous structure-activity relationships, a new series of potent CDK5 inhibitors was designed. This report describes the optimization of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.",

keywords = "6-Oxo-1,6-dihydropyridines, CDK5 inhibitor, Kinase, Neurodegenerative disorders",

author = "Kaller, \{Matthew R.\} and Wenge Zhong and Charles Henley and Ella Magal and Thomas Nguyen and David Powers and Rzasa, \{Robert M.\} and Weiya Wang and Xiaoling Xiong and Norman, \{Mark H.\}",

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doi = "10.1016/j.bmcl.2009.10.027",

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AU - Kaller, Matthew R.

AU - Zhong, Wenge

AU - Henley, Charles

AU - Magal, Ella

AU - Nguyen, Thomas

AU - Powers, David

AU - Rzasa, Robert M.

AU - Wang, Weiya

AU - Xiong, Xiaoling

AU - Norman, Mark H.

PY - 2009/12/1

Y1 - 2009/12/1

N2 - Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved in neurodegenerative disorders. Using active site homology and previous structure-activity relationships, a new series of potent CDK5 inhibitors was designed. This report describes the optimization of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.

AB - Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved in neurodegenerative disorders. Using active site homology and previous structure-activity relationships, a new series of potent CDK5 inhibitors was designed. This report describes the optimization of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.

KW - 6-Oxo-1,6-dihydropyridines

KW - CDK5 inhibitor

KW - Kinase

KW - Neurodegenerative disorders

UR - https://www.scopus.com/pages/publications/71749087776

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DO - 10.1016/j.bmcl.2009.10.027

M3 - Article

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AN - SCOPUS:71749087776

SN - 0960-894X

VL - 19

SP - 6591

EP - 6594

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 23

ER -

Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors

Abstract

Keywords

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