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Design and Development of Potential Therapeutic Agents for Use in Hormone Responsive Cancers
Contents
Abstract
Acknowledgments
Contents
List of Tables
List of Schemes
List of Figures
List of Abbreviations
List of Symbols
1. Introduction
1.1 Overview
1.2 Hormone Responsive Cancers
1.2.1 Breast Cancer
1.2.1.1 Breast Cancer Divisions
1.2.1.2 Treatment
1.2.2 Estrogens and Estrogen Receptors
1.2.3 Prostate Cancer
1.2.3.1 Treatment
1.2.3.2 Androgen Receptors and Breast Cancer
1.3 Selective Estrogen Receptor Modulators
1.3.1 Tamoxifen
1.3.2 Raloxifene
1.4 Analogue Based Drug Discovery
1.5 Flavanoids
1.5.1 Isoflavanoids
1.5.2 Pterocarpans
1.5.3 Glyceollins
1.6 Retinoic Acid Receptors
1.6.1 Pharmaceutical Relevance
1.6.2 Retinoic Acid Receptors and Breast Cancer
2. Glyceollin / Raloxifene Analog Library
2.1 Overview
2.2 Design of Target Libraries (Glyceollin Analogs)
2.2.1 Synthesis of Glyceollin I
2.2.2 Investigation into the alpha-Iodination Process
2.3 Glyceollin Analog Design
2.3.1 Linker Attachment
2.3.2 Target Library
2.4 Glyceollin / Raloxifene Model Libraries
2.4.1 Designing Model Libraries
2.4.2 Synthesis of Carboxylic Adducts for Model / Target Libraries
2.4.3 Esterifications
2.4.3.1 Mitsunobu Reaction
2.4.3.2 Steglich Esterification
2.4.4 Esterification of Model Targets
2.4.5 Synthesis of Model Targets via an Acid Chloride Route
2.5 Growth Inhibition Data
2.5.1 Standards, Glyceollins and Models in Growth Inhibition Assays for Breast and Ovarian Cancer Cells
2.5.2 Standards, Glyceollins and Models in Growth Inhibition Assays for Prostate Cancer Cells
2.6 Synthetic Summary and Structure Activity Relationships from Model Compounds
2.7 Synthesis of Glyceollin Targets
2.7.1 Overcoming Sterics
2.7.2 Alternate Esterification Methods
2.7.2.1 Yamaguchi Esterification
2.7.2.2 Corey-Nicolaou Macrolactonization
2.7.2.3 Mesylation
2.7.2.4 Re-evaluation of Esterification Attempts
2.8 Conclusions
3. X-ray Protein Models for Glyceollin Systems
3.1 Devising an Appropriate ERα Protein Model
3.2 Standards and Glyceollins in ERα Protein Models
3.3 Model Compounds and Glyceollin Analogs in ERα
3.4 Standards and Glyceollins in AR Protein Models
3.5 Model Compounds and Glyceollin Analogs in the AR
3.6 Conclusions
4. ‘GLY / GLO Click’ Library
4.1 Introduction
4.2 Library Design
4.2.1 Glyceollin / Glycinol Analog Library
4.2.2 Glyceollin / Glycinol Analog Model Library
4.3 Synthesis of Glyceollin / Glycinol Analog Model Compounds
4.4 Glyceollin / Glycinol Analog Target Synthesis
4.5 Docking Studies of Model and Glyceollin / Glycinol Targets
4.5.1 Docking Studies of Model and Glyceollin / Glycinol Target Compounds in ERα
4.5.2 Docking Studies of Model and Glyceollin / Glycinol Target Compounds in the AR
4.5.3 Molecular Modeling Conclusions
4.6 Conclusions
5. Retinoic Acid Receptors : A Secondary Target in Breast Cancer
5.1 Overview
5.2 Target Antagonist CD3-868
5.2.1 Molecular Model of CD3-868
5.3 Proposed Antagonist CD3-887
5.3.1 Molecular Model of CD3-887
5.4 Biological Studies of Targets
5.5 Conclusions
6. Experimental Details
6.1 Organic Chemistry Methods
6.1.1 Synthesis of Glyceollin I Intermediates
6.1.2 Synthesis of Glyceollin / Raloxifene Models
6.1.3 Synthesis of Glyceollin / Raloxifene Targets
6.1.4 Synthesis of GLY / GLO Models
6.1.5 Synthesis of GLY / GLO Click Targets
6.1.6 Synthesis of Retinoic Acid Receptor Intermediates and Targets
6.2 Biological Studies
6.2.1 Growth Inhibition Studies for Glyceollin Model Libraries
6.2.2 Luciferase Bioassay
6.3 Docking Studies
References 2
A. Spectra
B. Biological Data
C. Additional Molecular Models Bài viết liên quan
