Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.

Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. Research Abstract Details 

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Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. Abstract Text:

Robert M Rzasa,Matthew R Kaller,Gang Liu,Ella Magal,Thomas T Nguyen,Timothy D Osslund,David Powers,Vincent J Santora,Vellarkad N Viswanadhan,Hui-Ling Wang,Xiaoling Xiong,Wenge Zhong,Mark H Norman,Robert M Rzasa,Matthew R Kaller,Gang Liu,Ella Magal,Thomas T Nguyen,Timothy D Osslund,David Powers,Vincent J Santora,Vellarkad N Viswanadhan,Hui-Ling Wang,Xiaoling Xiong,Wenge Zhong,Mark H Norman,

Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in the early development of the nervous system. Deregulation of CDK5 is believed to contribute to the abnormal phosphorylation of various cellular substrates associated with neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Acyclic urea 3 was identified as a potent CDK5 inhibitor and co-crystallographic data of urea 3/CDK2 enzyme were used to design a novel series of 3,4-dihydroquinazolin-2(1H)-ones as CDK5 inhibitors. In this investigation we present our synthetic studies toward this series of compounds and discuss their biological relevance as CDK5 inhibitors.

Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. Publishing Authors By Initials

RM Rzasa,MR Kaller,G Liu,E Magal,TT Nguyen,TD Osslund,D Powers,VJ Santora,VN Viswanadhan,HL Wang,X Xiong,W Zhong,MH Norman,RM Rzasa,MR Kaller,G Liu,E Magal,TT Nguyen,TD Osslund,D Powers,VJ Santora,VN Viswanadhan,HL Wang,X Xiong,W Zhong,MH Norman,

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Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 6574-95

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 25

MONTH: 07

YEAR: 2007

Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. Information

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LANGUAGE: eng

NlmUniqueID: 9413298

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Grant and Affiliation Information for Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.

AFFILIATION: Department of Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1789, USA. rrzasa@amgen.com

Country: England

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MEDLINETA: Bioorg Med Chem

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