Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations

 

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dc.contributor.advisor Chibale, Kelly en_ZA
dc.contributor.advisor Caira, Mino R en_ZA
dc.contributor.author Melo, Candice Soares de en_ZA
dc.date.accessioned 2014-08-13T14:27:08Z
dc.date.available 2014-08-13T14:27:08Z
dc.date.issued 2006 en_ZA
dc.identifier.citation Melo, C. 2006. Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations. University of Cape Town. en_ZA
dc.identifier.uri http://hdl.handle.net/11427/6334
dc.description Includes bibliographical references. en_ZA
dc.description.abstract The work presented in this thesis is two-fold: (i) development of single agents that provide inhibition of both the growth of malaria parasites and of tumour cells in vitro, and (ii) inclusion of these potential novel inhibitors in cyclodextrin host molecules in an attempt to render these dual drugs water-soluble. Of all the current clinically established antimalarials, the 4-aminoquinolines haveproven to be the most significant and efficacious for the treatment and prophylaxis of malaria. However, their efficacy has decreased by the spread of drug resistant strains of the causative agent Plasmodium Jalciparum. Future research into 4-aminoquinoline derivatives as antimalarial agents is still warranted and justified on the basis of several considerations. The quinoline moiety has also been shown to be a substructure in multi-drug resistance reversal agents against certain cancer cell lines and antitumour agents which have demonstrated the ability to act as differentiation-inducing agents. The strategy employed for this project was to hybridize chalcone moieties and their Mannich base derivatives with the 4-aminoquinoline moiety. This dual drug concept uses the basic structure of the chalcone scaffold, which has a wide range of known antimalarial and anticancer activities, and is hybridised with the 4-aminoquinoline moiety, in order to exert maximal biological activity and overcome or prevent drug resistance. Structural variation on the aromatic rings of the chalcone scaffold allowed preliminary structure-activity relationship studies to be undertaken. en_ZA
dc.language.iso eng en_ZA
dc.subject.other Chemistry en_ZA
dc.title Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations en_ZA
dc.type Master Thesis
uct.type.publication Research en_ZA
uct.type.resource Thesis en_ZA
dc.publisher.institution University of Cape Town
dc.publisher.faculty Faculty of Science en_ZA
dc.publisher.department Department of Chemistry en_ZA
dc.type.qualificationlevel Masters
dc.type.qualificationname MSc en_ZA
uct.type.filetype Text
uct.type.filetype Image
dc.identifier.apacitation Melo, C. S. d. (2006). <i>Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations</i>. (Thesis). University of Cape Town ,Faculty of Science ,Department of Chemistry. Retrieved from http://hdl.handle.net/11427/6334 en_ZA
dc.identifier.chicagocitation Melo, Candice Soares de. <i>"Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations."</i> Thesis., University of Cape Town ,Faculty of Science ,Department of Chemistry, 2006. http://hdl.handle.net/11427/6334 en_ZA
dc.identifier.vancouvercitation Melo CSd. Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations. [Thesis]. University of Cape Town ,Faculty of Science ,Department of Chemistry, 2006 [cited yyyy month dd]. Available from: http://hdl.handle.net/11427/6334 en_ZA
dc.identifier.ris TY - Thesis / Dissertation AU - Melo, Candice Soares de AB - The work presented in this thesis is two-fold: (i) development of single agents that provide inhibition of both the growth of malaria parasites and of tumour cells in vitro, and (ii) inclusion of these potential novel inhibitors in cyclodextrin host molecules in an attempt to render these dual drugs water-soluble. Of all the current clinically established antimalarials, the 4-aminoquinolines haveproven to be the most significant and efficacious for the treatment and prophylaxis of malaria. However, their efficacy has decreased by the spread of drug resistant strains of the causative agent Plasmodium Jalciparum. Future research into 4-aminoquinoline derivatives as antimalarial agents is still warranted and justified on the basis of several considerations. The quinoline moiety has also been shown to be a substructure in multi-drug resistance reversal agents against certain cancer cell lines and antitumour agents which have demonstrated the ability to act as differentiation-inducing agents. The strategy employed for this project was to hybridize chalcone moieties and their Mannich base derivatives with the 4-aminoquinoline moiety. This dual drug concept uses the basic structure of the chalcone scaffold, which has a wide range of known antimalarial and anticancer activities, and is hybridised with the 4-aminoquinoline moiety, in order to exert maximal biological activity and overcome or prevent drug resistance. Structural variation on the aromatic rings of the chalcone scaffold allowed preliminary structure-activity relationship studies to be undertaken. DA - 2006 DB - OpenUCT DP - University of Cape Town LK - https://open.uct.ac.za PB - University of Cape Town PY - 2006 T1 - Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations TI - Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations UR - http://hdl.handle.net/11427/6334 ER - en_ZA


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