Literature DB >> 21420204

Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity.

Mahendra Shiradkar1, John Thomas, Vanita Kanase, Rajendra Dighe.   

Abstract

A novel clubbed triazolyl thiophene series of cdk5/p25 inhibitors, potentially useful for the treatment of Alzheimer's disease, is disclosed. Evaluation of the SAR of substitution within these series has allowed the identification of a range of compounds which significantly reduce brain cdk5/p25 and thus have potential as possible treatments for Alzheimer's disease.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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Year:  2011        PMID: 21420204     DOI: 10.1016/j.ejmech.2011.02.059

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Discovery of thienoquinolone derivatives as selective and ATP non-competitive CDK5/p25 inhibitors by structure-based virtual screening.

Authors:  Arindam Chatterjee; Stephen J Cutler; Robert J Doerksen; Ikhlas A Khan; John S Williamson
Journal:  Bioorg Med Chem       Date:  2014-09-28       Impact factor: 3.641

2.  Consensus models for CDK5 inhibitors in silico and their application to inhibitor discovery.

Authors:  Jiansong Fang; Ranyao Yang; Li Gao; Shengqian Yang; Xiaocong Pang; Chao Li; Yangyang He; Ai-Lin Liu; Guan-Hua Du
Journal:  Mol Divers       Date:  2014-12-16       Impact factor: 2.943

3.  Several human cyclin-dependent kinase inhibitors, structurally related to roscovitine, are new anti-malarial agents.

Authors:  Sandrine Houzé; Nha-Thu Hoang; Olivier Lozach; Jacques Le Bras; Laurent Meijer; Hervé Galons; Luc Demange
Journal:  Molecules       Date:  2014-09-23       Impact factor: 4.411

  3 in total

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