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Total synthesis of natural product pterocarpans useful as selective estrogen receptor modulators
Contents
Abstract
Acknowledgments
Contents
List of Tables
List of Figures
List of Schemes
List of Abbreviations
List of Spectra and Chromatograms
1 Introduction
1.1 Outline and Aim of Dissertation
1.2 Breast Cancer
1.3 Role of Estrogens and Estrogen Receptors in Breast Cancer
1.4 Selective Estrogen Receptor Modulators (SERMs)
1.5 Phytoestrogens
1.6 Isoflavonoids
1.6.1 Pterocarpans
1.6.1.1 6a-Hydroxypterocarpans
1.6.2 Phytoalexins
1.6.3 Glyceollins (GLYs)
1.7 Biological Testing of Compounds
2 Results and Discussion - Chemical Syntheses
2.1 Synthesis of 6a-Hydroxypterocarpans
2.1.1 Model Chemistry - Synthesis of Glycinol (GLO)
2.1.1.1 Biomimetic Synthesis
2.1.1.2 Non-Biomimetic Route
2.1.1.3 Synthesis via Intramolecular Benzoin Condensation
2.2 Synthesis of Glyceollin II (GLY II)
2.2.1 Retrosynthetic Strategy
2.2.2 Early Efforts and Results
2.2.3 Completion of Synthesis
2.3 Synthesis of Glyceollin III (GLY III)
2.3.1 Initial Retrosynthetic Strategy
2.3.2 Later Synthetic Efforts
2.3.3 Future Directions to Synthesis
2.4 Design and Synthesis of New Analogs Having Potential SERM Activity
2.4.1 Synthesis of Benzofuran Based Analogs
3 Results and Discussion - Molecular Modeling and Biological Studies
3.1 Molecular Modeling and Receptor Docking Studies
3.1.1 Development of Molecular Model for Estrogen Receptor
3.1.2 Analysis of Docking Studies for Glyceollins and Related Pterocarpans
3.1.3 Analysis of Docking Studies for Benzofuran Targets
3.2 Biological Evaluation of Intermediates and Final Compounds
3.3 Relative Correlation of Predicted Docking Scores with Experimental Data
3.4 Future Directions for Design and Development of Novel SERMs
3.5 Summary of Results for Syntheses and Pharmacological Properties of Glyceollins and Related Analogs
4 Experimental Details
4.1 General Experimental
4.2 Synthesis of Glycinol (GLO)
4.3 Synthesis of Glyceollin II (GLY II)
4.4 Synthesis of Glyceollin III (GLY III)
4.5 Synthesis of Benzofuran Analogs
4.6 Molecular Modeling
4.7 Biological Evaluation
References
Appendices
A. Additional Molecular Modeling and Recceptor Docking Results.
B. Measured GI50 Values of Standards and Tested Compounds for Breast, Ovarian and Prostate Cancer Cell Lines
C. Spectra and Chromatograms Bài viết liên quan
