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Derivatives of Amaryllidaceae alkaloids and their biological activity: Derivatives of tazettine II
Zelina, Dušan ; Cahlíková, Lucie (advisor) ; Špulák, Marcel (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Dušan Zelina Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivates of Amaryllidaceae alkaloids and their biological activity: Derivates of tazettine II Plants of family Amaryllidaceae are a rich source of alkaloids that are characterized by a broad biological activity. Perhaps the world's best-known member of this family has become galanthamine, which, because of its potent inhibitory potential, has found a place in the treatment of Alzheimer's disease. Based on the conducted studies, the alkaloid tazettine has been chosen for this thesis. The main purpose was to prepare more active derivatives of tazettine and to test the biological activity for potential use in the treatment of cancer and Alzheimer's disease. Ten aromatic esters of tazettine were prepared. Reaction yields ranged from 33,5-69,3 %. Derivatives were identified by MS, NMR and optical rotation. Prepared compounds were tested for their inhibitory potential against human cholinesterases - AChE and BuChE. Unfortunately, it has not been possible to prepare derivatives, which exhibit significant activity in inhibiting AChE or BuChE. Anti-tumor activity of the derivates has been tested on the panel of selected...
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Derivatives of Amaryllidaceae alkaloids and their biological activity: Derivatives of tazettine I
Pidaný, Filip ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Filip Pidaný Supervisor: Assoc. Prof. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae alkaloids and their their biological activity: Derivatives of tazettine I A study conducted between 1981 and 2014 found that 65% of small molecule based drugs are related to natural substances. The plants of the family Amaryllidaceae contain a particular and still not fully investigated group of alkaloids called Amaryllidaceae alkaloids. Their important biological effects include, for example, antiviral, antibacterial, antifungal, antiparasitic, cytotoxic and, in particular, motor-neuronal system-mediated effects mediated by inhibition of cholinesterases. A widespread Amaryllidaceae alkaloid is tazettine, a structural type alkaloid of tazettine that has increased interest in the early 1970s due to its cytotoxic acitivity, but appears less interesting in the studies conducted. The subject of this thesis was the preparation of tazettin alkaloid derivatives. The cholinesterase inhibitory activity was then tested. Cytotoxic activity in a panel of selected tumor and healthy cell lines was studied by screening. Unfortunately, none of the derivatives prepared by us showed an...
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Derivatives of Amaryllidaceae alkaloids and their biological activity: Derivatives of tazettine II
Zelina, Dušan ; Cahlíková, Lucie (advisor) ; Špulák, Marcel (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Dušan Zelina Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivates of Amaryllidaceae alkaloids and their biological activity: Derivates of tazettine II Plants of family Amaryllidaceae are a rich source of alkaloids that are characterized by a broad biological activity. Perhaps the world's best-known member of this family has become galanthamine, which, because of its potent inhibitory potential, has found a place in the treatment of Alzheimer's disease. Based on the conducted studies, the alkaloid tazettine has been chosen for this thesis. The main purpose was to prepare more active derivatives of tazettine and to test the biological activity for potential use in the treatment of cancer and Alzheimer's disease. Ten aromatic esters of tazettine were prepared. Reaction yields ranged from 33,5-69,3 %. Derivatives were identified by MS, NMR and optical rotation. Prepared compounds were tested for their inhibitory potential against human cholinesterases - AChE and BuChE. Unfortunately, it has not been possible to prepare derivatives, which exhibit significant activity in inhibiting AChE or BuChE. Anti-tumor activity of the derivates has been tested on the panel of selected...
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