Part 1 total synthesis and biological evaluation of antillatoxin and fragments part II synthetic studies towards the total synthesis of cytochalasans and tuberostemonine
Part 1 total synthesis and biological evaluation of antillatoxin and fragments part II synthetic studies towards the total synthesis of cytochalasans and tuberostemonine
... PART I TOTAL SYNTHESIS AND BIOLOGICAL EVALUATION OF ANTILLATOXIN AND FRAGMENTS PART II SYNTHETIC STUDIES TOWARDS THE TOTAL SYNTHESIS OF CYTOCHALASANS AND TUBEROSTEMONINE APPENDIX ... Biological Evaluation of Antillatoxin and Fragments 1. 1 Historical Background 1. 2 Previous Synthetic Studies 1. 3 Our Retrosynthetic Analysis of Antillatoxin 11 1. 4 Results and Discussion 15 1. 5 ... 1. 5 Biological Evaluation of Antillatoxin and Fragments Using Zebrafish Embryo 30 1. 6 Conclusion 44 1. 7 Experimental 45 Part II Chapter 2: Synthetic Studies Towards the Total Synthesis of Cytochalasans...
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Part i synthesis of photochromic fulgides part II synthetic studies towards anti SARS agent AG7088
... PHOTOCHROMIC FULGIDES 17 PART I CHAPTER Synthesis of Model Fulgides CHAPTER – SYNTHESIS OF FULGIDES 2.1 PRELIMINARY SYNTHESIS OF PHOTOCHROMIC FULGIDES As a preliminary investigation of the overall synthetic ... of increasing ring size on the photochromic properties of the fulgides PART I – SYNTHESIS OF PHOTOCHROMIC FULGIDES 30 PART I CHAPTER Synthesis of Cycloalkylidene Fulgides CHAPTER – SYNTHESIS OF ... PART I – SYNTHESIS OF PHOTOCHROMIC FULGIDES PART II – SYNTHETIC STUDIES TOWARDS ANTI- SARS AGENT AG7088 WAYNE LEE WEI WOON B.Sc (Hons.), NUS A THESIS SUBMITTED FOR THE DEGREE OF DOCTOR OF PHILOSOPHY...
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Part i synthesis and biological evaluation of phosphoglycolipid PGL1 analogues part II synthesis and biological evaluation of andrographolide analogues
... PART I SYNTHESIS AND BIOLOGICAL EVALUATION OF PHOSPHOGLYCOLIPID PGL1 ANALOGUES PART II SYNTHESIS AND BIOLOGICAL EVALUATION OF ANDROGRAPHOLIDE ANALOGUES HADHI WIJAYA (BSc (Hons.) NUS) A THESIS ... CONTENTS iv SUMMARY vii LIST OF TABLES ix LIST OF FIGURES xi LIST OF SCHEMES xv LIST OF ABBREVIATIONS xvii CHAPTER INTRODUCTION 1.1 Overview 1.2 Definition, Classification and sources of Natural Products ... treatment of various diseases In this thesis, the synthesis and biological evaluation of analogues of two natural products are presented In Chapter 2, the synthesis and biological evaluation of phosphoglycolipid...
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Solid phase synthesis and biological evaluation of 1, 3, 5 triazine derivatives
... 1,3 ,5- Triazine Derivatives 11 1.2.2 Synthesis of 1,3 ,5- Triazine Derivatives 14 1.2.2.1 Solution phase synthesis of 2,4,6-trisubtituted -1,3 ,5- triazine 14 1.2.2.2 Solid- Phase Synthesis of 1,3 ,5- Triazine ... 65 3.4 Synthesis of 1,3 ,5- triazine Analogs via Guanidium Azolides 80 3 .5 Synthesis of 1,3 ,5- traizine-2,4-diones 3-17 81 3 .5. 1 Solution -Phase synthesis of 3-17 81 3 .5. 2 Solid- Phase Synthesis of ... the synthesis of 1,3 ,5- triazine, 7476 this section will concentrate on the recent solution -phase and solid- phase syntheses of the 1,3 ,5- triazine derivatives 1.2.2.1 Solution phase synthesis of...
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design, synthesis, and biological evaluation of new anti-cancer nitrogen-containing combretastatins and novel cysteine protease inhibitors for the treatment of chagas
... Evaluation of New Anti-cancer Nitrogen-Containing Combretastatins and Novel Cysteine Protease Inhibitors for the Treatment of Chagas Rogelio Siles Mentor: Kevin G Pinney, Ph.D In an effort to combat ... Derivatives of Combretastatins A-1 and A-4 66 Synthesis of Cold Precursors of Radio-labeled Combretastatins CA-1 and CA-4 70 Synthesis of OXi8007 and a Nitrogen-Based Indole 75 Biological and Biochemical ... Biochemical Evaluation of Cysteine Protease Inhibitors: Novel Compounds for Chagas Disease Treatment 143 Introduction 143 Background 144 Chemotherapy of Chagas Disease 148 Chapter Seven: Materials and...
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Synthesis and biological evaluation of 2 substituted benzimidazole derivatives
... time in second (Mean ± SEM) 0h 2h 3h 4h 1.56 ± 0.16 2. 16 ± 0.16 2. 0 ± 0 .25 2. 16 ± 0.16 2. 0 ± 0 .25 2. 0 ± 0 .25 1.61 ± 0.30 2. 16 ± 0.30 2. 0 ± 0 .25 2. 16 ± 0.16 2. 0 ± 0 .25 2. 16 ± 0.16 Control Std 3a 3b ... 14.38; found C 57 .29 , H 3.65, N 14.45 Synthesis and biological evaluation of 2- substituted benzimidazole derivatives 2. 2 .2. 2 (1H-Benoimidazol -2- ylmethyl)- (2, 3-dichloro-phenyl)amine (3b) Light ... MS: 26 8 [M+]; Anal calcd for C14H12N4O2 (26 8): C 62. 68, H 4.51, N 20 .88; found C 62. 74, H 4.49, N 20 .78 2. 2 .2. 10 (1H-Benzimidazol -2- ylmethyl)-(4-iodo-phenyl)-amine (3j) Colorless powder; m.p .22 1 22 3...
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Synthesis and biological evaluation of isoindigo derivatives as anti proliferative agents
... functionalized isoindigos as antiproliferative agents, the aim of this thesis was to investigate medicinal chemistry approaches towards the design and synthesis of functionalized isoindigos with ... of isoindigos without compromising biological activity 1.5 Biological properties of functionalized isoindigos 1.5.1 Mode of action of meisoindigo Meisoindigo is the most widely investigated of ... understanding of the isoindigo scaffold and 19 to provide an objective assessment of its potential as a source of potent and drug-like compounds 20 Chapter 2: Functionalized isoindigos as cyclin-dependent...
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Synthesis and biological evaluation of natural products and their analogs as new cancer chemotherapeutic agents
... SYNTHESIS AND BIOLOGICAL EVALUATION OF NATURAL PRODUCTS AND THEIR ANALOGS AS NEW CANCER CHEMOTHERAPEUTIC AGENTS FANG ZHANXIONG (B.Sc.(Hons.) NUS) A THESIS SUBMITTED FOR THE DEGREE OF DOCTOR OF ... production of a large number of analogs with the basic template.56 Epothilone D has shown to be at least as cytotoxic as paclitaxel against a range of cancer cell lines and one of 15 the analogs has ... as anticancer agents due to their high selectivity against A549 cells In Chapter 3, the synthesis of lignan natural products as potential anti-tumor agents was described After the synthesis of...
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Design, synthesis and biological evaluation of inhibitors of flavivirus NS2B NS3 protease
... the thesis involves the design, synthesis and biological evaluation of inhibitors of Dengue and West Nile virus NS2B- NS3 protease For the design of dengue NS2B- NS3 protease inhibitors, we were inspired ... DEN2 NS2b- NS3 protease 60 Chapter 4: Synthesis and biological evaluation of small molecule inhibitors of West Nile Virus NS2B/ NS3 Protease 4.1 63 4.1.1 Chemistry 65 4.1.2 4.2 Introduction Biological ... kD VTA↓G, Unknown NS2B 14 kD RR↓S, NS2B- NS3 Protease NS3 70 kD RR↓S, NS2B- NS3 Protease NS4A 16 kD RR↓G, NS2B- NS3 Protease NS4B 28 kD VAA↓N, Signalase NS5 103 kD RR↓G, NS2B- NS3 Protease Function/enzymatic...
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Synthetic studies towards total synthesis of bielschowskysin 1
... lophotoxin and 11 pukalide x Scheme 1. 9 Marshall’s synthesis of the furan moiety of rubifolide 11 Scheme 1. 10 Marshall’s synthesis of furan moiety from an alkynone β-ketoester 11 Scheme 1. 11 Paquette’s ... Characterisation 1. 1.2 Biological Activity 1. 1.2 .1 Antimalarial Agents and Continuing Needs 1. 1.3 Proposed Biosynthesis 1. 1.4 Related Diterpene Natural Products 1. 1.5 Relevant Synthetic Efforts 1. 1.5 .1 Butenolide ... iv 1. 1.5.2 Furan Construction 10 1. 1.5.3 Macrocycle Construction 12 1. 1.6 Sulikowski’s Synthetic Study 14 1. 2 Approaches toward Related Diterpenes 1. 2 .1 Leo Paquette Approach 15 1. 2.2 Marshall...
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Synthetic studies towards total synthesis of bielschowskysin 2
... natural products, we have begun studies towards the total synthesis of Our approach is to mimic the biosynthesis of by the [2+ 2] photo-cycloaddition of allenyl -2( 5H)furanone 157 under high stereocontrol ... stereocontrol to form the tricyclic core27 (Figure 2. 1) Figure 2. 1: Proposed model study of the tricyclic core of bielschowskysin 2. 2 Model Study: [2+ 2] Cycloaddition of Allene-Butenolide As an intramolecular ... Et2O BuOOH 93 O 94 H2 C 1-bromo -2- butyne C CH 95 (COCl) 2, DMSO CH Cl2 , Et3 N, -78 °C HO DIBAL-H O AgNO3 , acetone SnCl2 , NaI, DMPU H 3CO2 C H 3CO2 C 96 97 CBr , PPh3 OHC O Et 3N, CH 2Cl2 O...
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Part i organic reactions in non conventional solvents part II new approach to the formation of bishomoallylic alcohols synthesis of (r) sulcatol
... liquid, 15 Cl 14 Scheme The newly designed ionic liquid 15 Summary vii Part II: New Approach to the Formation of Bishomoallylic Alcohols – Synthesis of (R)- Sulcatol The regioselectivitives of ... Efficient Chemical Kinetic Resolution of Bishomoallylic Alcohols: Synthesis of (R )Sulcatol Publication List Table of Contents 187 216 iv Summary Part I: Organic Reactions in Non- Conventional Solvents ... Application of Mannich bases and their derivatives in medicine Hence, the versatility of the Mannich reaction, along with the remarkable possibilities of exploiting the reactivity of Mannich bases in...
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Synthetic studies towards sieboldine a and a macrocyclic precursor of bielschowskysin
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