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Synthesis and biological evaluation of isoindigo derivatives as anti proliferative agents

Synthesis and biological evaluation of isoindigo derivatives as anti proliferative agents

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 2 substituted benzimidazole derivatives

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 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

... 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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Solid phase synthesis and biological evaluation of 1, 3, 5 triazine derivatives

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

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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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

... 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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Design, synthesis and biological evaluation of inhibitors of flavivirus NS2B NS3 protease

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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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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Synthesis and biological investigation of pyrimido 1,2 a 1,3,5 triazine and its analogues 2

Synthesis and biological investigation of pyrimido 1,2 a 1,3,5 triazine and its analogues 2

... Methionine aminopeptidase Translation, ribosomal structure and biogenesis 2ea2, 1boa, 2gg8, 2p98, 2g6p 2. 948 0.58 62 43 1-aminocyclopropane-1carboxylate deaminase Amino acid transport and metabolism ... hepatocyte growth factor activity 3f 82, 3cd8 2. 956 0 .27 23 Branched-chain-amino-acid aminotransferase, mitochondrial Amino acid transport and metabolism 1kta, 1kt8 2. 94 0 .26 24 Renin Renin is a ... Met- and Leu-enkephalins by cleavage of a Gly-Phe bond 1r1i, 1y8j 3 .29 8 0.3548 3.644 0 .22 58 17 20 21 Amino acid transport and metabolism 22 DNA polymerase I, thermostable Replication, recombination...
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Synthesis and biological investigation of pyrimido,1,2 a ,1,3,5,triazine and its analogues 1

Synthesis and biological investigation of pyrimido,1,2 a ,1,3,5,triazine and its analogues 1

... derivatives Anti-fungal activity was stated for derivatives 10 1a against Microsporum canis and average affinity of 10 1b for serotoninergic 5-HT 1A and 5-HT2B receptors was also published by Lucry and ... cyclocondensation of biguanide and its analogues 13 2 with ethyl acetoacetate gave 12 8 -13 1 as reported by Curd and Rose92 (Scheme 39, Method A) There was a need to develop an alternative method of obtaining ... catalyzed cyclization of potassium N,N-dicyanobenzamidine 11 2 with methyl anthranilate 11 1 in methanol gave triazino[2 ,1- b]quinazolone 11 4 instead of triazino [1, 2 -a] quinazolone 11 4’ In order to confirm...
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Design, synthesis and biological studies of coumarin based probes and tetrahydrolipstatin analogs 1

Design, synthesis and biological studies of coumarin based probes and tetrahydrolipstatin analogs 1

... NBD-sarcosine (1. 14) and 7-dimethylamino coumarin- 4-acetic acid (1. 15).9 R O R O MeO O O O H O O O O O O O O O 1. 12 R = OAc 1. 16 R = 1. 14 1. 17 R = 1. 15 O2 N 1. 13 R = OAc 1. 18 R = 1. 14 1. 19 R = 1. 15 N N ... F Eur Pat 19 98, EP08479 91 13 Paterson, M J.; Jovanovic, A Arkivoc, 2 010 , 10 , 11 -16 14 Nielsen, O.; Burchardt, O Synthesis, 19 91, 819 -8 21 15 Dey, B B J Chem Soc 19 15, 10 7, 16 06 -16 51 16 (a) Pederson, ... enantiosynthesis of THL 54 4 .11 Kumaraswamy’s synthesis of THL 56 4 .12 Synthesis of β-hydroxy aldehyde 4. 71 57 4 .13 Davies’ synthesis of THL 57 4 .14 Raghavan’ synthesis of THL 59 4 .15 Hanson’ synthesis of...
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Design, synthesis and biological studies of coumarin based probes and tetrahydrolipstatin analogs

Design, synthesis and biological studies of coumarin based probes and tetrahydrolipstatin analogs

... 125.7577890 MHz DATE_d : DECNUC : off NS 39.9955 39.8279 39.7551 39.6968 39.6603 39.4927 39.3324 39.1648 38.9972 38.8514 38.7057 BF1 : 137 Oct 23 2006 NUCLEUS : off PULPROG : zgpg30 SFO1 : 125.7709936 ... Parameters *** O sg1023~1 : *** Acquisition Parameters *** O 2.19 Oct 23 2006 : off NS O : DECNUC N : 125.7577890 MHz DATE_d : 57 off PULPROG : N H BF1 NUCLEUS : N H (1) N O : PROCNO 34.0345 33.9106 O ... MHz 1.00 Hz 32768 *** 1D NMR Plot Parameters *** O N H (1) 35.0 : SF 60 50 40 30 20 10 60.62 Hz off 220 39.6968 38.8514 38.7057 38.4506 34.0345 33.9106 69.5313 69.4875 68.9774 68.9556 97.4419...
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Synthesis and reactivity studies of cyclopentadienyl derivatives of ruthenium iridium and osmium iridium mixed metal clusters 5

Synthesis and reactivity studies of cyclopentadienyl derivatives of ruthenium iridium and osmium iridium mixed metal clusters 5

... C6H5), 1 .59 (s, 15H, 5. 05s 25 1974sh, 1948w Cp*), -13. 95 (dd, 1H, 2JP-H = 11 .55 Hz; JHH = 3.3 Hz, OsHOs), -16.87 (d, 1H, JHH = 3.3 Hz, IrHOs) 2060vs, 2005sh, 1991vs, 7.83-7.76 (m, 15H, C6H5), ... structure and refinement data are given in Tables 5. 5 and 5. 6 193 Table 5. 2 Experimental conditions used for the synthesis of compounds 23-26 Products and isolated yields Amount of Amount of PPh3Se ... 1371.9 658 1377. 958 51 29 .50 29.70 2.20 2. 25 1464.80 14 65. 35 - - - - 151 4.8414 151 4.84 252 2024vs, 2008m, 2000m, = 3.3 Hz, OsHOs), -16.90 (d, 1H, 2JHH 1989s, 1967w, 1 950 m = 3.3 Hz, IrHOs) 2 057 s, 2038vs,...
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Synthesis and reactivity studies of cyclopentadienyl derivatives of ruthenium iridium and osmium iridium mixed metal clusters 1

Synthesis and reactivity studies of cyclopentadienyl derivatives of ruthenium iridium and osmium iridium mixed metal clusters 1

... bridging one face of the cluster (Figure 1. 1) Ir Ir Rh Ir Ir Rh Rh Rh Figure 1. 1 Comparison of tetranuclear clusters of Ir4(CO )12 and Rh4(CO )12 The low solubility of Ir4(CO )12 and Rh4(CO )12 in organic ... to ligands and substrates As the focus of the research is on the synthesis and reactivity of mixed metal carbonyl clusters, a short review of some of the ligands like CO, hydrides, and cyclopentadienyls ... cluster anions and mono- or di-nuclear metal cations Clegg and coworkers have reported the synthesis of penta and hexanuclear mixed- metal clusters Os4Rh(μ-H2)(CO )13 and Os4Rh2(μ-H)2(CO )11 (η5-Cp*)2...
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Synthesis and reactivity studies of cyclopentadienyl derivatives of ruthenium iridium and osmium iridium mixed metal clusters 2

Synthesis and reactivity studies of cyclopentadienyl derivatives of ruthenium iridium and osmium iridium mixed metal clusters 2

... Os(3) 2. 7644(4) 2. 9148(3) 2. 9061(4) 2. 7077 (2) Ir(1)- Os(4)/(3A) 2. 7 326 (3) 2. 9148(3) 2. 78 62( 16) 2. 76 52( 6) 2. 924 6(3) Os (2) - Os(3) 2. 9656(4) 2. 8013(4) Ru (2) -Ru(4)/(3A) 2. 8990(17) 2. 76 52( 6) 2. 8765(3) ... CpRhOs3(μ-H )2( CO)10 20 83m, 20 63vs, 20 42vs, 20 10vs, 20 00s(sh), 1982m, 1972m, 1819m Cp*RhOs3(μ-H )2( CO)10 20 84m, 20 64s, 20 41s, 20 02s, 1969w, 1962w, 1792m 41 Figure 2. 6 ORTEP diagram of Cp*IrOs3(μ-H )2( CO)10, ... Cp*IrOs3(μ-H )2( CO)10 (3c) 2. 7789(4) 2. 7644(4), 2. 7 326 (3) Cp*RhOs3(μ-H )2( CO)10 2. 769(1) 2. 769(1), 2. 734(1) CpIrOs3(μ-H )2( CO)10 2. 798(1) 2. 749(1), 2. 740(1) CpRhOs3(μ-H )2( CO)10 2. 736 (2) 2. 730(1), 2. 729 (1)...
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