Aurones as chemosensors

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Table of contents

1. General introduction
References
2. Aurones
2.1 General introduction
2.2 Synthesis of aurone derivatives
2.3 Aurones and their role in colouring flowers
2.4 Aurones as fluorescent probes with potential applications
2.5 Aurones as chemosensors
2.6 Biological roles, targets and activities
i. Aurones as antiparasitic agents
ii. Aurones as antimicrobial agents
iii. Aurones as anti-viral agents
iv. Aurones as anti-inflammatory agents
v. Aurones as anti-cancer agents
vi. Aurones to treat skin diseases
vii. Aurones in Alzheimer’s disease
viii. Aurones as SIRT1 inhibitors
ix. Aurones as potential biological herbicides
x. Aurones as radical scavenger
2.7 Summary of the literature survey
2.8 Novel benzopyran-2- and 4-one-containing aurones
2.8.1 Chemistry
2.8.2 Biology
2.9 Conclusion and Outlook
2.10 Experimental part
2.10.1 Chemistry
2.10.1.1 General introduction
2.10.1.2 Synthesis of the aurone derivatives
2.10.2 Biology
2.10.2.1 General
2.10.2.2 Cell culture
2.10.2.3 Cell Cycle Analysis on K562 Cells
2.11 References
3. DNMT Inhibitors
3.1 Introduction to Epigenetics
3.2 DNA methyltransferases
3.2.1 General introduction
3.2.1 Catalytic mechanism of DNMTs
3.3 Known DNMT inhibitors
3.3.1 Nucleoside-like inhibitors
3.3.2 Non-nucleoside inhibitors
3.4 Summary of the literature survey
3.5 Optimisation study SGI 1027
3.5.1 Chemical synthesis of compounds 84-96
3.5.2 Biochemical and biological results
3.5.2.1 DNMT1, DNMT3A2/3L, PRMT1 and GLP assays
3.5.2.2 Docking studies of compound 84 and 88 as well as mechanism of action of 88
3.5.2.3 Effects of quinoline-based DNMTi in a panel of cancer cell lines.
3.5.2.4 Effects of 85 and 88 in medulloblastoma stem cells (MbSCs)
3.6 Conclusion and outlook
3.7 Experimental part
3.7.1 Chemistry
3.7.1.1 General introduction
3.7.1.2 Synthesis of selective non-nucleosidic human DNMTi
3.7.2 Biology
3.7.2.1 General introduction
3.7.2.2 Nanoscale DNMT1 pre-screen. HotSpot DNMT assay
3.7.2.3 DNMT1, DNMT3A2/3L, PRMT1, and GLP inhibition assays
3.7.2.4 DNMT1 inhibition assay
3.7.2.5 DNMT3A inhibition assay
3.7.2.6 PRMT1 and GLP inhibition assays
3.7.2.7 Competition studies
3.7.2.8 Molecular modelling
3.7.2.9 U-937, RAJI, PC-3, MDA-MB-231 and PBM cellular assays
3.7.2.10 Medulloblastoma cancer stem cell (MbSC) assays
3.7.2.11 RNA isolation and Real-Time qPCR
3.7.2.12 Western blot assay
3.7.2.13 MTT assay
3.8 References
4. Coumarin based chalcones as potential NF-κB inhibitors
4.1. General introduction
4.2. Chemistry
4.3. Effect of synthetic coumarin-based molecules on the TNF-alpha induced NF-κB pathway
4.4. Conclusion and outlook
4.5. Experimental part
4.5.1 Chemistry
4.5.1.1 General introduction
4.5.1.2 Synthesis of potential NF-κB inhibitors
4.5.2 Biology
4.5.1.3 General introduction
4.5.1.4 Cell culture
4.5.1.5 Assay to test the TNF-alpha induced NF-κB pathway
4.6. References
5. Conclusion and perspectives
6. French summary
6.1. Introduction
6.2. Les aurones
6.3. Les inhibiteurs de la méthyltransférase de l’ADN
6.4. Chalcones à base de coumarine comme des inhibiteurs potentiels de NF-κB
6.5. Conclusion et perspectives
6.6. References