Design, synthesis and biological evaluation of bioorganometallic metallarectangles
type: CreativeWork
description: Malaria is a devastating mosquito-borne disease, characterized by high levels of morbidity and mortality. The absence of a suitable vaccine to offer protection and the emergence of drug-resistant parasite strains continues to be the driving force behind the development of new antimalarial agents. Cancer, which is the second leading cause of deaths globally, accounted for a estimated 9.6 million deaths in 2018. Despite tremendous advances made within the field of drug discovery, the past four decades of cancer chemotherapeutic treatment has largely depended on platinum-based drugs (e.g. cisplatin and its derivatives). Unfortunately, the use of these metallodrugs are accompanied by severe adverse side-effects. Additionally, the evolution of resistant cancer cell sub-types has rendered many of these highly efficacious platinum drugs, ineffective. Utilizing alternative platinum group metals (PGMs), such as iridium and ruthenium, and incorporating known pharmacophoric scaffolds within the framework of a target compound, has been a favourable approach toward combating these obstacles, while further enhancing the pharmacological activity of potential drug candidates. The increased popularity and success of metal-containing compounds as pharmaceutical agents has prompted investigations into the pharmacological activity of a different class of metal-based compounds, supramolecular coordination complexes (SCCs). Such complexes have been extensively investigated for their anticancer activity, with many PGM SCCs displaying activity greater than or comparable to available clinical chemotherapeutic drugs. Interestingly, however, no studies have investigated the antiplasmodial activity of SCCs, a field that warrants further exploration. Due to the pharmacological activity associated with the quinoline scaffold, this pharmacophore was incorporated into a newly designed N,N'-ditopic ligand (L). The quinoline-containing ligand (L), synthesized via a Suzuki cross-coupling reaction, wa…
abstract: Malaria is a devastating mosquito-borne disease, characterized by high levels of morbidity and mortality. The absence of a suitable vaccine to offer protection and the emergence of drug-resistant parasite strains continues to be the driving force behind the development of new antimalarial agents. Cancer, which is the second leading cause of deaths globally, accounted for a estimated 9.6 million deaths in 2018. Despite tremendous advances made within the field of drug discovery, the past four decades of cancer chemotherapeutic treatment has largely depended on platinum-based drugs (e.g. cisplatin and its derivatives). Unfortunately, the use of these metallodrugs are accompanied by severe adverse side-effects. Additionally, the evolution of resistant cancer cell sub-types has rendered many of these highly efficacious platinum drugs, ineffective. Utilizing alternative platinum group metals (PGMs), such as iridium and ruthenium, and incorporating known pharmacophoric scaffolds within the framework of a target compound, has been a favourable approach toward combating these obstacles, while further enhancing the pharmacological activity of potential drug candidates. The increased popularity and success of metal-containing compounds as pharmaceutical agents has prompted investigations into the pharmacological activity of a different class of metal-based compounds, supramolecular coordination complexes (SCCs). Such complexes have been extensively investigated for their anticancer activity, with many PGM SCCs displaying activity greater than or comparable to available clinical chemotherapeutic drugs. Interestingly, however, no studies have investigated the antiplasmodial activity of SCCs, a field that warrants further exploration. Due to the pharmacological activity associated with the quinoline scaffold, this pharmacophore was incorporated into a newly designed N,N'-ditopic ligand (L). The quinoline-containing ligand (L), synthesized via a Suzuki cross-coupling reaction, wa…
author: Golding, Taryn
keywords: Chemistry
date published: 2021
date modified: 2026-07-22T22:22:42Z
provider: University of Cape Town
publisher: Networked Digital Library of Theses and Dissertations
type: WebPage
source organization: Department of Chemistry

PropertyValue
property ID: Handle
value: http://hdl.handle.net/11427/35784