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1

Simpson, Grant J. "Quinone derivatives as novel single-molecule components for nano-electronics." Thesis, University of St Andrews, 2014. http://hdl.handle.net/10023/6309.

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In this thesis, quinone derivative molecules supported on a Cu(110) surface are studied using scanning tunnelling microscopy (STM). The experimentally investigated system is based on the bistable nature of these compounds, and so the work is introduced in the wider context of molecular electronics (Chapter 1). The theory and experimental techniques are also described (Chapters 2 and 3). In Chapter 4 the switching behaviour of azophenine (AP) and azotolyline (AT) is characterised using STM imaging and spectroscopy, and is demonstrated to be based on a hydrogen tautomerisation reaction. The acti
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2

Meye, Biyogo Alex. "Stratégie radicalaire SRN1/Mn(OAc)3 sur des dérivés naphtoquinoniques à visée pharmacologique." Thesis, Aix-Marseille, 2016. http://www.theses.fr/2016AIXM4750.

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Ce travail est consacré à la recherche et au développement de nouvelles molécules à viséepharmacologique en série naphtoquinonique en utilisant des réactions par transfert monoélectroniquede type SRN1 et des cyclisations radicalaires oxydatives induites par l'acétate de manganèse(III). Lapremière partie décrit l’étude de la réactivité SRN1 de la 2-(chlorométhyl)-3-méthoxynaphtoquinoneavec divers anions nitronates conduisant à la formation de produits de C-alkylation avec de bonsrendements. Ces derniers ont fait l’objet d’une réaction de réduction-cyclisation permettant la synthèsede nouveaux d
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3

Haddad, Jalal. "Synthesis and chemistry of some quinoline-5,8-diones." Virtual Press, 1994. http://liblink.bsu.edu/uhtbin/catkey/917048.

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The synthesis of several 7-substituted analogs of 2-methylquinoline-5,8-dione and their chemistry are described. In this investigation the following compounds were prepared.5,7-Diformamido-8-hydroxy-2-methylquinoline (207), 7-formamido-2methylquinoline-5,8-dione (199), 7-acetamido-2-methylquinoline-5,8-dione (6), 7-isobutyramido-2-methylquinoline-5,8-dione (200), 7-amino-2-methylquinoline-5,8-dione (210), 7-amino-6-chloro-2-methylquinoline-5,8-dione (213), 7-methoxy-2-methylquinoline5,8-dione (214), 7-ethoxy-2-methylquinoline-5,8-dione (215), 7-isopropyloxy-2methylquinoline-5,8-dione (216), 7-
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4

Ahmad, Abid Rafiq. "Studies of novel diazanaphthoquinones and ion-responsive fluorescent quinoxaline derivatives." Thesis, Brunel University, 1994. http://bura.brunel.ac.uk/handle/2438/7130.

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The work reported is divided into two parts: fIrstly a section dealing with the preparation of some novel diazanaphthoquinones and their reactions, especially the Diels-Alder reaction, and secondly an account of some quinoxaline derivatives and their fluorescence properties. Quinoxaline quinones containing electron-donating groups at both the 2- and 3- position have shown a difference in their stability and their behaviour in the Diels-Alder reaction compared to the stability and the reactions of quinoxaline quinone. Symmetrical dienes in the Diels-Alder reaction yielded the initial addition p
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5

Klaas, Phindile Jonathan. "Novel approaches to the synthesis of quinoline derivatives." Thesis, Rhodes University, 2001. http://hdl.handle.net/10962/d1004751.

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The investigation has been concerned with the application of the Baylis-Hillman methodology to the synthesis of quinoline derivatives. An extensive range of novel Baylis-Hillman products has been prepared, typically in moderate to excellent yields, by condensing 2-nitrobenzaldehyde derivatives with various vinyl ketones and acrylic esters in the presence of diazabicyclo[2.2.2]octane (DABCO). Reduction of the nitro group in the Baylis-Hillman products was effected by catalytic hydrogenation in ethanol using a 10% palladium-on-carbon catalyst to afford quinoline, quinoline-N-oxide and quinolone
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6

Ijaz, A. S. "The synthesis of oxindole and isatin derivatives with potential radiosensizer activity." Thesis, Brunel University, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.378349.

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7

Pakade, Vusumzi Emmanuel. "Application of the Baylis-Hillman reaction in the preparation of quinoline derivatives." Thesis, Rhodes University, 2006. http://hdl.handle.net/10962/d1007669.

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The reaction of various 2-nitrobenzaldehyde derivatives with methyl vinyl ketone (MVK) in the presence of 1,4-diazabicyclo[2.2.2]octane (DABCO) has afforded the Baylis-Hillman adducts in moderate to good yield. Dissolution of the catalyst in the solvent before the addition of the aldehyde was observed to improve the yield. Reduction of the Baylis-Hillman adducts was effected by catalytic hydrogenation using a 10% palladium-on- carbon catalyst in ethanol to give quinoline and quinoline-N-oxide derivatives and, in some cases, acyclic reduction products. All products were characterised using NMR
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8

Meye, Biyogo Alex. "Stratégie radicalaire SRN1/Mn(OAc)3 sur des dérivés naphtoquinoniques à visée pharmacologique." Electronic Thesis or Diss., Aix-Marseille, 2016. http://www.theses.fr/2016AIXM4750.

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Ce travail est consacré à la recherche et au développement de nouvelles molécules à viséepharmacologique en série naphtoquinonique en utilisant des réactions par transfert monoélectroniquede type SRN1 et des cyclisations radicalaires oxydatives induites par l'acétate de manganèse(III). Lapremière partie décrit l’étude de la réactivité SRN1 de la 2-(chlorométhyl)-3-méthoxynaphtoquinoneavec divers anions nitronates conduisant à la formation de produits de C-alkylation avec de bonsrendements. Ces derniers ont fait l’objet d’une réaction de réduction-cyclisation permettant la synthèsede nouveaux d
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9

Loke, P. L. "Chemoenzymatic and chemical synthesis of enantiopure quinoline derivatives and alkaloids." Thesis, Queen's University Belfast, 2003. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.273295.

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10

Sharma, A. K. "Studies towards antitumor quinoline derivatives and development of useful synthetic methodologies." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2001. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/2319.

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11

Kgokong, Joseph Lebese. "Trifluoromethyl-substituted quinoline and tetrazole derivatives :design, synthesis, antimalarial activity and cytotoxicity / Joseph L. Kgokong." Thesis, North-West University, 2008. http://hdl.handle.net/10394/3732.

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Malaria is a complex parasitic disease caused by the Plasmodium falciparum. It has been found to be responsible for the death of many people particularly in under-developed and developing countries. For many years chloroquine and quinine have been the mainstay of therapy for this disease. The research on new therapies against malaria have been hampered by factors such as the development of resistance against these and some of the new drugs or combinations thereof, the lack of adequate knowledge on the exact causes and mechanisms of resistance to the drugs and their mode of action, together wit
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12

Ding, Ying. "Gap junction enhancer as an anti-cancer agent via GJIC-independent and -dependent pathways." Diss., Kansas State University, 2013. http://hdl.handle.net/2097/15705.

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Doctor of Philosophy<br>Department of Biochemistry and Molecular Biophysics<br>Thu Annelise Nguyen<br>Gap junctions (GJ) are intercellular channels connecting adjacent cells, allowing small molecules to transport between cells, thereby maintaining all homeostasis. Loss of gap junctional intercellular communication (GJIC) and/or connexins, the gap junction proteins, is a hallmark of cancer. Restoration of GJIC and/or increase of connexin expression have been related to the reduction of tumorigenesis. Connexins have been reported as tumor suppressors due to both GJIC-independent and -dependent m
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13

He, Li. "Synthesis of C-D-glycopyranosyl benzo(hydro)quinones and glycosyl derivatives of tocopherols, as enzyme inhibitors or antioxidants, and investigation of a new α-glycosylation". Lyon 1, 2007. http://www.theses.fr/2007LYO10208.

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: Les C-glycosides sont des mimes résistants et utiles pour l’étude des glyco-enzymes. La réaction de Friedel-Crafts acido-catalysée entre le 1,4-diméthoxybenzène et des sucres peracétylés (D-gluco, D-galacto) conduit sous contrôle thermodynamique à des motifs C-glycosylés de configuration béta. Ils ont été oxydés en glycosyl-benzoquinones qui, réduites en hydroquinones, conduisent à diverses glycosyl-hydro(benzo)quinones acétylées ou non. Pour des raisons stériques et électroniques, les isomères ortho-, et méta-diméthylés du 1,4-diméthoxybenzène sont réactifs lors de substitutions électrophil
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14

Tukulula, Matshawandile. "The design and synthesis of novel HIV-1 protease inhibitors." Thesis, Rhodes University, 2009. http://eprints.ru.ac.za/1563/.

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15

Leung, Suet Ching. "New and established drug targets for malaria chemotherapy from lead optimisation of 2-pyridyl quinolone PfNDH2 inhibitors to semi-synthetic pyrrole Mannich base artemisinin derivatives." Thesis, University of Liverpool, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.577488.

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The rapid development of resistance to currently deployed antimalarial drugs has raised the desperate need for new chemotherapies, preferably with novel therapeutic target. This thesis explores the synthesis of novel quinolone compounds and artemisinin derivatives targeting the mitochondrial electron transfer chain (ETC) and the haemoglobin degradation of Plasmodium falciparum respectively. The respiratory chain of the human malaria is an attractive target for antimalarial drugs. It is believed that the collapse of the mitochondrial potential will shut down the metabolism and malaria parasite
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16

Gadakh, S. K. "Enantioselective synthesis of bioactive molecules and development of synthetic methodologies involving formation of quinoline and coumarin derivatives via Rh-catalyzed ortho C-H bond activation of aromatics." Thesis(Ph.D.), CSIR-National Chemical Laboratory, 2015. https://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/5939.

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Enantioselective Synthesis of Bioactive Molecules and Development of Synthetic Methodologies Involving Formation of Quinoline and Coumarin Derivatives via Rh-Catalyzed ortho C-H Bond Activation of Aromatics Research Student: Sunita K. Gadakh AcSIR Roll: 10CC11J26017 Research Guide: Dr. A. Sudalai The thesis entitled “Enantioselective Synthesis of Bioactive Molecules and Development of Synthetic Methodologies Involving Formation of Quinoline and Coumarin Derivatives via Rh-Catalyzed ortho C-H Bond Activation of Aromatics’’ is divided into four chapters. The title of the thesis clearly refle
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17

Lee, Yi-Chen. "Studies towards the development of novel HIV-1 integrase inhibitors." Thesis, Rhodes University, 2010. http://hdl.handle.net/10962/d1005022.

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The project has focused on the preparation of several series of compounds designed as potential HIV-1 integrase inhibitors. Various 2-nitrobenzaldehydes have been reacted with two activated alkenes, methyl vinyl ketone (MVK) and methyl acrylate, under Baylis-Hillman conditions to afford α-methylene-β-hydroxylalkyl derivatives in moderate to excellent yields. The reactions were conducted using the tertiary amine catalysts, 1,4-diazabicyclo[2.2.2]octane(DABCO) or 3-hydroxyquinuclidine (3-HQ) with chloroform as solvent, and yields were optimised by varying the catalyst, reagent concentrations and
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18

Bakhouya, Abderrahmane. "Etude du processus de libération des principes actifs à partir de formes galéniques lipidiques à matrice de gélucire : modélisation de la pénétration tissulaire de la ciprofloxacine." Saint-Etienne, 1996. http://www.theses.fr/1996STET4013.

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Les formes galéniques matricielles, à matrice lipidique tels que les gélucires, permettent une libération contrôlée du principe actif. Ces matrices peuvent subir une érosion plus ou moins prononcée selon la nature de l'excipient. Lorsque le gélucire est hydrophile, le processus de libération s'effectue par érosion de la forme galénique. Avec un gélucire lipophile, le processus de libération est contrôlé par diffusion. Pour simuler le contrôle de la libération par érosion dans l'organisme, nous avons construit un modèle numérique qui tient compte de tous les facteurs ; notamment, les trois stad
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19

Cardoso, Leandro 1979. "Utilização farmacológica de um composto inédito derivado de quinazolina como inibidor potencial da quinase de adesão focal (FAK) no processo de hipertrofia cardíaca em camundongo = Pharmacological use of a novel compound quinazoline derivative as potential inhibitor of the focal adhesion kinase in the process of cardiac hypertrophy in mice." [s.n.], 2012. http://repositorio.unicamp.br/jspui/handle/REPOSIP/310205.

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Orientador: Kleber Gomes Franchini<br>Dissertação (mestrado) - Universidade Estadual de Campinas, Faculdade de Ciências Médicas<br>Made available in DSpace on 2018-08-20T23:08:02Z (GMT). No. of bitstreams: 1 Cardoso_Leandro_M.pdf: 3831901 bytes, checksum: 40e5df211d7e6fd923f654bd8d3a1ec1 (MD5) Previous issue date: 2012<br>Resumo: Nas doenças do coração ocorre hipertrofia e remodelamento do ventrículo esquerdo com impacto negativo na evolução clínica. Esses fatores influenciam independentemente o risco cardiovascular por elevarem a predisposição a infartos do miocárdio, ao desenvolvimento de
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20

Benaissa, Tahar. "Synthèse de ligands contenant un atome de fluor et pouvant donner des complexes à applications médicales : étude de la complexation de la 5-fluoro-8-hydroxyquinoline avec des cations métalliques, par RMN du fluor." Université Joseph Fourier (Grenoble), 1996. http://www.theses.fr/1996GRE10100.

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Ce travail se place a la convergence de deux grands themes etudies au laboratoire: le marquage de molecules par un atome de fluor et l'etude de la complexation de cations metalliques par des ligands. La premiere partie concerne la preparation de deux series de ligands contenant du fluor: des biphenols et des composes contenant des groupements 2-fluoropyridines. Les biphenols substitues par deux ou quatre atomes de fluor (en position 4,4' ; 5,5' ; 4,4 ;,5,5') ont ete obtenus a partir de bromophenols par une reaction de type ullman. Leurs derives sulfones ont egalement ete prepares pour augmente
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21

HUANG, YU-LUN, and 黃煜倫. "Synthesis of calix[4]quinone derivatives." Thesis, 2017. http://ndltd.ncl.edu.tw/handle/22c3rn.

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碩士<br>中國文化大學<br>化學系應用化學碩士班<br>105<br>alixarenes, which are cyclic oligomers of p-substituted phenols and formaldehyde, are able to include small organic molecules or metal ions within the molecular cavities to form “host-guest” complexes. These phenomena have been proposed in the applications of micro-analysis, ion separation, and enzyme-mimic studies. The main purpose of this thesis is to study the synthesis of p-hydroxycalix[4]arene and its acetate derivatives. In the basic condition, p-tert-butylphenol were polymerized with formaldehyde to form a yellowish precursor. Refluxing of this precu
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22

Rozek, Tomas. "Biologically active natural products: ochromycinone analogues and aurein peptides : a thesis presented for the degree of Doctor of Philosophy / by Tomas Rozek." 2000. http://hdl.handle.net/2440/19824.

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Includes copies of articles co-authored by the author during preparation of this thesis.<br>Includes bibliographical references (leaves 185-191).<br>v, 192 leaves : ill. ; 30 cm.<br>Title page, contents and abstract only. The complete thesis in print form is available from the University Library.<br>Sixteen aurein peptides are present in the host defence secretion from the granular dorsal glands of the Green and Golden Bell Frog (Litoria aurea) and seventeen from those of the related Southern Bell Frog (Litoria raniformis). All peptides have been sequenced using a combination of electrospray m
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23

Yu, Tzer-Shun, and 余澤順. "The Study of the Calix[4]quinone Ether Derivatives." Thesis, 2003. http://ndltd.ncl.edu.tw/handle/25896368459025456304.

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碩士<br>中國文化大學<br>應用化學研究所<br>91<br>Calixarenes, which are cyclic oligomers of p-substituted phenols and formaldehyde, are able to include small organic molecules or metal ions within the molecular cavities to form ‘‘ host-guest ’’ complexes. These phenomena have been proposed in the applications of micro- analysis, ion separation, and enzyme-mimic studies. The main purpose of this thesis is to study the oxidative ability of chlorine dioxide toward the calix[4]arene dialkyl ether derivatives. In the presence of a base, p-tert-butylphenol and formaldehyde were polymerized to form an ye
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24

Yang, Darlene, and 楊德琳. "Regulation of quinone reductase by indole derivatives from cruciferous vegetables." Thesis, 2000. http://ndltd.ncl.edu.tw/handle/17413079071222860623.

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碩士<br>台北醫學院<br>保健營養學研究所<br>88<br>Abstract The indoles, such as indole-3-carbinol (I3C) and indolo[3,2-b]carbazole (ICZ), are thought to be the bioactive components in cruciferous vegetables. The induction of detoxification enzymes, such as quinone reductase ( QR ), is closely associated with the chemopreventive effect of various phytochemicals. The present study was aimed to study the role of I3C and ICZ on the regulation of QR in both murine (Hepa1) and human (HepG2) hepatoma cells. The results showed that ICZ is a potent QR inducer, but its parent compound, I3C, had no significant
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25

Ni, Xiang-Ru, and 倪湘茹. "Triazole Functionalized Calix[4]quinone Derivatives as Highly Selective Ion Sensor." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/86db3z.

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碩士<br>國立交通大學<br>應用化學系碩博士班<br>104<br>In this study, we modified the lowerrim of the calix[4]arene by attaching distal pyrene unit as the fluorophore through the click chemistry of pyrene azides with 25, 27bispropargyl calix[4]arene. Based on the methods developed by Ms. YingJung Chen, we successfully synthesized the unique skeleton of calix[4]quinone and its derivatives 3336. Based on the results from UVVis spectroscopy and fluorescence spectrometry, we found that fluorescence emission intensity decreased, because more flexible structure will cause energy lost in the cases of 33; 34 posses
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26

Chang-YouSie and 謝昌佑. "Synthesis of Acridines and Azepines from 1,4- Quinone Derivatives via Free Radical Reaction and Electrophilic Reaction." Thesis, 2017. http://ndltd.ncl.edu.tw/handle/4xv5z6.

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碩士<br>國立成功大學<br>化學系<br>105<br>SUMMARY The methods which use free radicals for cyclization reaction can be found in many literatures. Herein we used sulfonyl radical with the compounds that contain triple bond in the presence of silver(I) nitrate and potassium persulfate via the oxidative free radical cyclization reaction to synthesis benzo[b]acridine derivatives. Surprisingly, we found that azepine derivatives were produced as the by-products under certain conditions. So we divided the reaction into two steps to synthesis benzo[b]naphtho[2,3-f]azepine derivatives alone. Keywords: silver(I) nit
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27

Huang, Shi-Zong, and 黃仕宗. "Preparation of Various Quinone Derivatives with the Assistance of Silver Carbonate via C-H Functionalization and Leads to the Formations of C-N and C-P Bonds." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/b9xdm5.

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碩士<br>國立中興大學<br>化學系所<br>104<br>In this work, the synthesis and characterization of several quinone derivatives with specific configurations were described. Stoichiometric amount of silver carbonate was employed and the C-H activation on the quinone was observed. Crystal structures of several newly-made quinone derivatives were determined by X-ray diffraction methods. These novel quinone derivatives having both phosphine group(s) and amine functional group(s) might act as P,N-bidentate ligands toward transition metals and form metal-containing pre-catalysts. The potential of these pre-catalysts
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28

KO, DEN-YUAN, and 柯登淵. "Synthesis of Quinoline Derivatives of Curcumin." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/02939843223114971684.

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碩士<br>中國文化大學<br>化學系應用化學碩士班<br>104<br>Curcumin is isolated from the rhizome of Curcuma longa. Much evidence indicated that curcumin could be used as a therapeutic agent in the treatment of Alzheimer’s disease (AD) and could reduce the symptoms, including oxidative damage, inflammation, senile plaques, neurofibrillary tangles, cell cycle dysregulation and neuron damages. AD, a complex disease with multiple etiological factors, needs a multifunctional drug forits treatment. Curcumin is one of the potential drugs in the treatment of AD. Some quinolines are known as good metal chelating agents
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29

Chen, Ping-Cheng, and 陳柄成. "Synthesis of 2-Phenyl-4-Quinolone Derivatives." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/87206938834357809645.

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碩士<br>國立成功大學<br>化學系碩博士班<br>97<br>Compounds isolated from natural products containing a heterocyclic ring represent an important class of biologically active molecules that are widespread in nature. Organic chemists have reported many methods for the total synthesis of these compounds. In our laboratory, we are interested in the synthesis of 2-phenyl-4-quinolone derivatives due to their anticancer activity. On the other hand, these derivatives showed the poor solubility in water and organic solvent. In order to solve this problem, we designed to synthesize these derivatives by Mannich reaction
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30

Teitgen, Alicen M. "Novel synthesis of quinoline-5,8-dione analogues." 2012. http://liblink.bsu.edu/uhtbin/catkey/1678996.

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The chemistry of quinonline-5,8-dione as a functional group is a developing field because of its various biological aspects. Lavendamycin and streptonigrin are known antibiotic, antitumor agents containing the quinolone-5,8-dione functional group believed to provide their antitumor properties. Most cancer cells show an elevated level of NQO1 enzyme which activates lavendamycin to act as an antitumor agent. The research goal is to explore different synthetic methods and reactions to produce novel quinolone-5,8-dione analogues with unique structural features while keeping the selective cytotoxic
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31

Fang, Kuo-Chang, and 方國璋. "Synthesis, Antibacterial, and Cytotoxic Evaluation of Quinolone Derivatives." Thesis, 2001. http://ndltd.ncl.edu.tw/handle/20909424944491902243.

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博士<br>高雄醫學大學<br>藥學研究所<br>89<br>Although the structure-activity relationships of antibacterial fluoroquinolones have been extensively investigated, the optimum substituent at C-7 position which has a great impact on potency, spectrum, solubility and pharmacokinetics has not been precisely defined. The present study describes the preparation and evaluation of certain norfloxacin derivatives with an additional functional moiety such as 4-hydroxyaminoalkyl (R-C=N-OH) on the C-7 piperazin-1-yl group, with the aim of providing extra hydrogen-bonding capabilities with the target DNA gyrase and theref
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32

Pors, Klaus, Z. Paniwnyk, Laurence H. Patterson, K. C. Ruparelia, J. A. Hartley, and L. R. Kelland. "Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells." 2004. http://hdl.handle.net/10454/3164.

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No<br>Novel 1- and 1,4-substituted chloroethylaminoanthraquinones with DNA binding and alkylating properties along with their respective hydroxyethylaminoanthraquinone intermediates were synthesized. Selected chloroethylaminoanthraquinones were shown to cross-link DNA and alkylate guanines (at low nM concentration) with a preference for reaction sites containing 5'-PyG. A compound (Alchemix) with the bis-chloroethyl functionality confined to one side chain alkylated but did not cross-link DNA. All the 1,4-disubstituted chloroethylaminoanthraquinones were potently cytotoxic (nM IC50s) against c
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33

Lin, Bao-Jiun, and 林保君. "Synthesis and Biological Evaluation of Furo[3,2-h]quinoline and Furo[2,3-h]quinoline Derivatives." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/61262624727227638045.

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碩士<br>大仁科技大學<br>製藥科技研究所<br>97<br>Certain aniline- or phenoxy-substituted furo[3,2-h]quinolin-8-yl, furo[2,3-h]quinolin-2-yl, and 7-prop-2-ynyloxyquinolin-2-yl derivatives were synthesized and evaluated for their anti-inflammatory activities. These compounds were synthesized via alkylation of hydroxyl precursors followed by the chlorination, cyclization, and reaction with appropriate Ar-NH2 or Ar-OH. Anti- inflammatory activities of these quinoline derivatives were evaluated on the suppression of reactive oxygen species (ROS) production induced by formyl-methionyl-leucyl-phenylalanine (fMLP, 1
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34

Martins, Sandra Cristina Cardoso. "The anticancer potential of CITme, a quinoline derivative." Diss., 2011. http://hdl.handle.net/2263/26129.

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3-[3-(7-chloro-quinolin-4-yl amino) phenyl]-1-(4-methoxy-phenyl) prop-2-enone citrate “CITme” is a substituted quinoline derivative, synthesized as a potential antitumour agent. The aim of this study was to investigate CITme with regard to antitumour activity, toxicity and pharmacokinetics. In vitro screening for neoplastic cytotoxic effects using standard cell culture techniques revealed cytotoxic activity against HeLa, DU-145, MCF-7, Jurkat and CoLo 320 human derived cancer cell lines at low concentrations. Toxicity was significantly less in either normal resting and stimulated lymphocytes o
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Hung, Chia, and 蒲家弘. "1-Arylpyrrolo[3,2-c]quinoline Derivatives as Potential Anticancer Agents." Thesis, 2010. http://ndltd.ncl.edu.tw/handle/24584162853152668729.

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碩士<br>靜宜大學<br>應用化學研究所<br>99<br>This thesis is aimed at design and synthesis of 1-arylpyrrolo[3,2-c]quinoline derivatives as potential anticancer agents. We had been using quinoline ring as skeleton for the design of 1-arylpyrrolo[3,2-c]quinoline derivatives to force the two aromatic rings in cis conformations. Results of in vitro cytotoxicity presumed that this series of compounds have potentials as anticancer drugs. In this study, we change substituent on aryl ring to prepare a series new 1-arylpyrrolo[3,2-c]quinoline derivatives. The synthesis was initiated from the condensation of appropria
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36

Yang, Chiao-Li, and 楊巧麗. "Synthesis and Biological Evaluation of Benzofuro[2,3-b]quinoline Derivatives." Thesis, 2010. http://ndltd.ncl.edu.tw/handle/46052568130848169814.

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博士<br>高雄醫學大學<br>藥學研究所<br>98<br>Planar polyfused heteroaromatic compounds have various biological activities such as anticancer, antibacterial and antiviral effects. A series of 11-alkoxylated and 11-aminated benzofuro[2,3-b]quinoline derivatives were designed, synthesized, and evaluated for their anti-TB and cytotoxic activities. The known 11-chlorobenzofuro[2,3-b]quinoline (62) was synthesized in situ from anthranilic acid and 2-coumaranone in phosphorus oxychloride in 51% yield for the first time. Treatment of 62 with alcohols and amines gave 11-alkoxylated and 11-aminated benzofuro[2,3-b]q
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Lin, Ming-Nan, and 林明楠. "Synthesis and Biological Evaluation of Indeno[1,2-b]quinoline Derivatives." Thesis, 2008. http://ndltd.ncl.edu.tw/handle/11110602183432189459.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所<br>96<br>Synthesis and antiproliferative evaluation of 11H-indeno[1,2-b]quinoline derivatives with the structural characteristics of DNA intercalator are described. The results of this study indicate that the cytotoxic effect depends on the basic side chains that substituted in the planar nucleus of 11H-indeno[1,2-b]quinoline. Substituents at C-10 and C-11 positions are crucial to the antiproliferative potency of 11H-indeno[1,2-b]quinoline, the aminoalkoxyimino substitutent of10-methyl-11H-indeno[1,2-b]quinolin-11-one (8c-h), 11-oxo-11H-indeno[1,2-b]quinoline-10-carb
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38

Xie, You-Tern, and 謝宥騰. "Amberlyst 15-Promoted Improved Synthesis of Quinoline and Imide Derivatives." Thesis, 2008. http://ndltd.ncl.edu.tw/handle/07304571302598657970.

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碩士<br>高雄醫學大學<br>藥學研究所<br>96<br>Amberlyst 15 is a solid acid of catalytic agent, by the advantage it is easy to isolate and remove, and have no volatility and corrosiveness. Amberlyst 15 can be to recycle and used again, and will not pollute the environment. Compared with metal Lewis acid catalyst being the environmental protection even more, and comparatively cheap too.  Quinoline and its derivatives display a wide spectrum of biological activities such as antimalarial, antibacterial, antidiabetic, and anti-inflammatory.  Imide derivatives constitute an important class of organic compounds wit
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39

Tseng, Chih-Hua, and 曾志華. "Synthesis and Biological Evaluation of Indeno[1,2-c]quinoline Derivatives." Thesis, 2008. http://ndltd.ncl.edu.tw/handle/15724151089081379022.

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博士<br>高雄醫學大學<br>藥學研究所<br>96<br>Although the quinoline ring is found in a wide variety of biologically active compounds and is frequently condensed with various heterocycles, synthesis and biological evaluation of the indenoquinoline skeleton attracts only very limited attention. Synthesis of certain indeno[1,2-c]quinoline derivatives (formula I) wherein R1 represents hydrogen and halide; R2 represents hydrogen, halide, hydroxy, alkylamino, arylamino, cyclic alkylamino such as piperazine, morpholine and their substituted derivatives; R3 represents hydrogen, hydroxy, and alkylamino. R4 represent
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Wei, Yin-Ling, and 魏吟玲. "Design and Synthesis of Quinoline Derivatives as Potential Cytotoxic Agents." Thesis, 2005. http://ndltd.ncl.edu.tw/handle/60126835714289198157.

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碩士<br>國立臺灣大學<br>藥學研究所<br>93<br>The aim of this thesis is to design and synthesize quinoline derivatives as potential cytotoxic agents. Two series of target compounds, 3-phenylquinolines (7-10) and 2-phenylquinolines (11-14, 17 and 18), were prepared and evaluated for their cytotoxicity. In the preparation of 3-phenylquinolines 7-10, the required intermediates 8-nitro-3-phenylquinoline (1a) and 3-(4-methoxyphenyl)-8-nitroquinoline (1b) were obtained from 8-nitroquinoline by bromination with N-bromosuccinimide (NBS) followed by Suzuki coupling reaction. Reduction of the nitro compounds 1a,b with
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41

Shu, Yi-Ling, and 徐宜伶. "1-Arylpyrrolo[3,2-c]quinoline Derivatives as Potential Anticancer Agents." Thesis, 2010. http://ndltd.ncl.edu.tw/handle/69079911972583018314.

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碩士<br>靜宜大學<br>應用化學研究所<br>98<br>This thesis is aimed at design, synthesis, and evaluation of anticancer activity of 1-arylpyrrolo[3,2-c]quinoline derivatives. Combrestastatin A4 (CA-4) is a tubulin polymerization inhibitor, and its structural features possess two aryl rings containing methoxy groups in the cis form. Quinoline derivatives possess various biological activities in many aspects. It was used for the design of 1-arylpyrrolo[3,2-c]quinolines to force two aryl rings in cis form. In this study, we introduced substituents on the quinoline of 1-arylpyrrolo[3,2-c]quinoline derivatives. The
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Chen, Yu-Liang, and 陳昱良. "Synthesis and Biological Evaluation of Indolo[3,2-c]quinoline Derivatives." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/77952279380878195727.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所碩士班<br>95<br>Synthesis and antiproliferative evaluation of 11H-indolo[3,2-c]quinoline derivatives with the structural characteristics of DNA-intercalator are described. 11H-Indolo[3,2-c]quinoline is a coplanar tetracyclic heterocycle in which the consisting 2-phenyl- naphthalene are conformationally locked through a nitrogen bridge. The results of this study indicate that the cytotoxic effect depends on the basic side chains inserted in the planar nucleus of 11H-indolo[3,2-c]quinoline. The O-alkyloximes substituted of indoloquinoline derivatives(3e, 3f, 3g, 5c), which
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Wu, Jian-Long, та 吳建隆. "Ionic liquid promoted synthesis of α-azidoketones and quinoline derivatives". Thesis, 2007. http://ndltd.ncl.edu.tw/handle/16603925226947001269.

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碩士<br>高雄醫學大學<br>藥學研究所碩士班<br>95<br>Room temperature ionic liquids (RTIL) are liquids that are composed entirely of ions. In fact, ionic liquids can now be produced which remain liquid at room temperature and below (even as low as -90℃) and can be appeared to be undemanding and inexpensive to manufacture. Ionic liquids offer an attractive alterative to conventional organic liquids for clean synthesis, as they are recycling easily, lacking flammability, and possessing no vapour pressure effectively. Comparing with classical molecular solvents, the ionic liquids are environmentally benign reaction
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44

曹雪雄. "Synthesis and Application of Mono(Di)-Methine Quinoline Heterocyclic Derivatives." Thesis, 1997. http://ndltd.ncl.edu.tw/handle/01104416602051339795.

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碩士<br>國立臺灣科技大學<br>纖維及高分子工程技術研究所<br>85<br>In this study, Synthesis and application of Mono(Di)-methine quinoline heterocyclic derivatives. Quinoline was reacted with ethyl(amyl) iodide to give 1-substituted-2(4)-methyl quinoline, resulted in producing a series of Mono(Di)-methine and Aza- methine quinoline heterocyclic derivatives. In part one, quinoline was condensed with terephthalaldehyde to give a series of Di-methine quinoline derivatives, which leads to a series of violet to purplish blue coloured. In part two, quinoline was condensed with heterocyclic compounds of keton structur
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Jian, Zhenxing, and 簡振興. "1-Aryltriazolo[4,5-c]quinoline Derivatives As Potential Anticancer Agents." Thesis, 2012. http://ndltd.ncl.edu.tw/handle/27734992176570584849.

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碩士<br>靜宜大學<br>應用化學系<br>100<br>This thesis is aimed at design and synthesis of 1-aryltriazolo[4,5-c]quinoline derivatives as potential anticancer agents. Combrestastatin A4 (CA-4) is a tubulin polymerization inhibitor, and quinoline derivatives are known to possess biological activities in many aspects. Thus, quinoline skeleton was chosen for the design of 1-aryltriazolo[3,2-c]quinoline derivatives to force the two aromatic rings in cis conformations as those in CA-4. Condensation of anthranilic acids with 2-nitroacetaldehyde oxime resulted in 2-(2-nitroethylideneamino)benzoic acid (2), which w
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46

Wu, Cheng-Hsin, and 吳政炘. "Synthesis of Indeno[1,2-c]quinoline Derivatives as Antituberculosis Agents." Thesis, 2012. http://ndltd.ncl.edu.tw/handle/87358627783172486464.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所<br>100<br>The first-line drugs currently used for the treatment of tuberculosis (TB) infection are streptomycin, isoniazid (INH), ethambutol, pyrazinamide, and rifampicin. However, the current TB treatment regimens, although highly effective, are far from ideal. Recently, the emergence of multi-drug resistant (MDR) strains and the global human immunodeficiency virus (HIV) pandemic have created an urgent need for alternative drug treatments for Mycobacterium tuberculosis infection. Over the past few years, we have been particularly interested in the synthesis of conde
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47

Lo, Wei Fen, and 羅偉棻. "Synthesis and anticancer evaluation of 4-anilinofuro[2,3-b]quinoline and 4-anilinofuro[3,2-c]quinoline derivatives." Thesis, 2015. http://ndltd.ncl.edu.tw/handle/fyfqj3.

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博士<br>高雄醫學大學<br>醫藥暨應用化學系博士班<br>103<br>Certain furo[2,3-b]quinoline and furo[3,2-c]quinoline derivatives have been synthesized and evaluated for their antiproliferative activities. Among them, CIL-102 was found to be the most potent. However, it exhibited general cytotoxicity to most of cancers and normal cells. In addition, it displayed other drawbacks such as low oral availability and poor aqueous solubility. In order to improve these drawbacks, we optimized the chemical structure of CIL-102 to settle these problems. CIL-102 is active against the growth of PC-3、A549, MCF-7 and M-10 cells with
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48

Murali, Dheeptha. "Chemistry of quinoline-2-carbaldehyde derivatives with malononitrile and formation of indolizines." 2011. http://liblink.bsu.edu/uhtbin/catkey/1657738.

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The quinoline-5,8-diones are an important class of compounds with a wide spectrum of biological activites such as antibacterial, antiasthmatic, antifungal, antitumour and antiparasitic agents. Over the past three decades many variously substituted derivatives of quinoline-5,8-diones have been synthesized and reported. The majority of them dealt with the chemistry of C-6 and/or C-7 substituted quinolinediones and were related to Lavendamycin. Our lab has developed several procedures for the condensation (Knoevenagel) and reduction of aldehydes and ketones with malononitrile. When this reductive
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Chung, Kuin-Yu, and 鍾昆宇. "Synthesis and Cytotoxic Evaluation of 6-Arylindeno[1,2-c]quinoline Derivatives." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/38733413069967985944.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所<br>97<br>This thesis describes the synthesis and cytotoxic evaluation of 6-arylindeno[1,2-c]quinoline derivatives. The synthesized compounds were evaluated for their antiproliferative activities against liver cancers including Hep 3B、Hep G2、Hep 2.2.1 cell lines and lung caners including A549、H1299 cell lines. The results of this study indicated that the introduction of fluoro group at C-2 position significantly enhanced antiproliferative potency. The introduction of basic side chains on the tetracyclic pharmacophore improved selectivity against cancer cells. For exam
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50

Li, Shu-Yu, and 黎淑雲. "Synthesis and Cytotoxic Evaluation of Certain Pyrido[3,2-g]quinoline Derivatives." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/29517969036062887881.

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博士<br>高雄醫學大學<br>藥學研究所博士班<br>95<br>The present report describes the synthesis and evaluation of tricyclic pyrido[3,2-g]quinoline derivatives in which an additional pyridine ring is linearly fused on the antibacterial quinoline-3-carboxylic acid. Among them, only both diethyl 4, 6- diamino -10- methylpyrido- [3,2-g]quinoline-3,7-dicarboxylate (9a) and diethyl 4,6-bis-(3-dimethyl- aminopropylamino) -10- methylpyrido[3,2-g]quinoline-3,7-dicarboxylate (9d) were able to inhibit cell proliferation of MCF-7 (Breast), NCI-H460 (Lung), and SF-268 (CNS) implying either amino or dimethylaminopropyl moiety
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