Matching Items (2)
Filtering by
- All Subjects: Quinone
- Creators: Arce Amezquita, Pablo M
- Creators: Williams, Peter
Description
Mitochondria produce most of the ATP needed for the cell as an energy source. It is well known that cellular respiration results in oxidative damage to the cell due to the production of reactive oxygen species (ROS). Mitochondrial dysfunction is believed to contribute to a number of degenerative diseases; because of this the mitochondrial respiratory chain is considered as potential drug target. A few series of idebenone analogues with quinone, pyridinol and pyrimidinol redox cores have been synthesized and evaluated as antioxidants able to protect cellular integrity and, more specifically, mitochondrial function. The compounds exhibited a range of activities. The activities observed were used for the design of analogues with enhanced properties as antioxidants. Compounds were identified which provide better protection against oxidative stress than idebenone, and it is thought that they do so catalytically.
ContributorsArce Amezquita, Pablo M (Author) / Hecht, Sidney M. (Thesis advisor) / Moore, Ana (Committee member) / Rose, Seth (Committee member) / Arizona State University (Publisher)
Created2012
Description
Many natural and synthetic quinones have shown biological and pharmacological activity. Some of them have also shown anticancer activity. Ubiquinone (CoQ10) which is a natural quinone, is a component of the electron transport chain and participates in generation of ATP (adenosine triphosphate). Cellular oxidative stress is key feature of many neurodegenerative diseases such as Friedreich's ataxia, Alzheimer's disease and Parkinson's disease. The increased generation of reactive oxygen species damages cell membranes and leads to cell death. Analogues of ubiquinone in the form of pyrimidinols and pyridinols, were effective in protecting Friedreich's ataxia lymphocytes from oxidative stress- induced cell death. There were some structural features which could be identified that should be useful for the design of the analogues for cellular protection against oxidative stress. There are quinones such as doxorubicin, daunomycin and topopyrones which have anticancer activity. Here I evaluated topopyrone analogues which poison both topoisomerases I and II. The topopyrone analogues were lethal to human breast cancer cells, but these analogues were not as potent as camptothecin.
ContributorsRaghav, Nidhi (Author) / Hecht, Sidney M. (Thesis advisor) / Gould, Ian R (Committee member) / Williams, Peter (Committee member) / Arizona State University (Publisher)
Created2011