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Design, Synthesis, and Evaluation of Functionalized Chroman-4-one and Chromone Derivatives. Somatostatin receptor agonists and Sirt2 inhibitors


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Title: Design, Synthesis, and Evaluation of Functionalized Chroman-4-one and Chromone Derivatives. Somatostatin receptor agonists and Sirt2 inhibitors
Authors: Fridén-Saxin, Maria
E-mail: saxin@chem.gu.se
Issue Date: 4-Oct-2012
University: University of Gothenburg. Faculty of Science
Institution: Department of Chemistry ; Institutionen för kemi
Parts of work: I. Synthesis of 2-Alkyl-Substituted Chromone Derivatives Using Microwave Irradiation Fridén-Saxin, M., Pemberton, N., Andersson, K. S., Dyrager, C., Friberg, A., Grøtli, M., Luthman, K. Journal of Organic Chemistry 2009, 7, 2755–2759.
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II. KHMDS Enhanced SmI2-mediated Reformatsky Type α-Cyanation Ankner, T., Fridén-Saxin, M., Pemberton, N., Seifert, T., Grøtli, M., Luthman, K., Hilmersson, G. Organic Letters 2010, 12, 2210-2213.
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III. Substituted Chroman-4-one and Chromone Scaffolds: Design, Synthesis, and Evaluation of Somatostatin β-Turn Mimetics Fridén-Saxin, M., Seifert, T., Andersson, K. S., Pemberton, N., Dyrager, C., Friberg, A., Dahlén, K., Wallén, E. A. A., Grøtli, M., Luthman, K. Unpublished manuscript.

IV. Synthesis and Evaluation of Substituted Chroman-4-one and Chromone Derivatives as Sirtuin 2 Selective Inhibitors Fridén-Saxin, M.,† Seifert, T.,† Rydén Landergren, M., Suuronen, T., Lahtela-Kakkonen, M. L., Jarho, E. M., Luthman, K. Journal of Medicinal Chemistry 2012, 55, 7104-7113.
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V. Chroman-4-one Based Inhibitors of Sirtuin 2 with Antiproliferative Effects Seifert, T., Fridén-Saxin, M., Engen, K., Kokkola, T., Wallén, E. A. A., Suuronen, T., Lahtela-Kakkonen, M. L., Jarho, E. M., Luthman, K. Unpublished manuscript.

VI. Proline Mediated Formation of Novel Chroman-4-one Tetrahydropyrimidines Fridén-Saxin, M., Seifert, T., Hansen, L.K., Grøtli, M., Erdelyi, M., Luthman, K. Tetrahedron 2012, 68, 7035-7040.
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Date of Defence: 2012-11-01
Disputation: Torsdagen den 1 november, kl 9.00, Hörsal KC, Hörsalsvägen 2
Degree: Doctor of Philosophy
Publication type: Doctoral thesis
Keywords: Chroman-4-ones
Chromones
Inhibitors
Molecular Modeling
Peptidomimetic
Samarium
Sirtuin
Sirt2
Somatostatin
Structure-Activity Relationships
Tubulin
β-Turn
Abstract: Peptides are involved in many physiological processes such as regulation of blood-pressure, food intake, pain transmission and blood-glucose levels. They consist of amino acids that are connected through amide bonds which make peptides hydrophilic and conformationally flexible. Peptides generally make poor oral drugs as amide bonds are easily cleaved by endogenous enzymes. One way to overcome the structural problems with peptides is to develop stabilized mimetics, so called peptidomimetics, via ... more
ISBN: 978-91-628-8548-9
URI: http://hdl.handle.net/2077/30223
Appears in Collections:Doctoral Theses from University of Gothenburg / Doktorsavhandlingar från Göteborgs universitet
Doctoral Theses / Doktorsavhandlingar Institutionen för kemi och molekylärbiologi

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