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

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dc.contributor.advisorChibale, Kellyen_ZA
dc.contributor.advisorCaira, Mino Ren_ZA
dc.contributor.authorMelo, Candice Soares deen_ZA
dc.date.accessioned2014-08-13T14:27:08Z
dc.date.available2014-08-13T14:27:08Z
dc.date.issued2006en_ZA
dc.descriptionIncludes bibliographical references.en_ZA
dc.description.abstractThe 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.identifier.apacitationMelo, 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/11427/6334en_ZA
dc.identifier.chicagocitationMelo, 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/11427/6334en_ZA
dc.identifier.citationMelo, C. 2006. Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations. University of Cape Town.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
dc.identifier.urihttp://hdl.handle.net/11427/6334
dc.identifier.vancouvercitationMelo 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/11427/6334en_ZA
dc.language.isoengen_ZA
dc.publisher.departmentDepartment of Chemistryen_ZA
dc.publisher.facultyFaculty of Scienceen_ZA
dc.publisher.institutionUniversity of Cape Town
dc.subject.otherChemistryen_ZA
dc.titleAnti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigationsen_ZA
dc.typeMaster Thesis
dc.type.qualificationlevelMasters
dc.type.qualificationnameMScen_ZA
uct.type.filetypeText
uct.type.filetypeImage
uct.type.publicationResearchen_ZA
uct.type.resourceThesisen_ZA
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