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Identifier 000460149
Title Σύνθεση βιοδραστικών ενώσεων με πιθανή αντικαρκινική δραστικότητα
Alternative Title Synthesis of bioactive compounds with potential anticancer activity
Author Γαλάτης-Βαξοβάνος, Κωνσταντίνος
Thesis advisor Κώστας, Ιωάννης
Reviewer Μαγουλάς, Γεώργιος
Πίντζας, Αλέξανδρος
Abstract In this research work, new bioactive compounds were synthesized, which aim to inhibit the action of BRAF. In particular, three compounds, which were designed in previous studies of our laboratory, were synthesized and gave promising results in biological studies. Mutated BRAF occurs in several common types of cancer, including colorectal, non-small cell lung cancer, thyroid cancers, and a significant majority of melanomas. The majority of cancers arising from mutated BRAF are due to the V600E mutation within the kinase. The mutated protein kinase prevents cell apoptosis, leading to uncontrolled cell proliferation and development of cancer cell survival mechanisms. BRAF inhibitors must selectively target cancer cells, based on the genetics of the tumor, while at the same time having little effect on normal cells, thus limiting the side effects that traditional treatment techniques such as chemotherapy and radiotherapy include. The synthesized compounds contain a sulfonamide group, but also the benzothiazole functional group. Many commercial drugs are benzothiazole derivatives, as these scaffolds possess a variety of pharmacological activities, including antiviral, antimicrobial, diuretic, anti-inflammatory, anticancer, and antioxidant properties. All three compounds formed contain at one end the sulfonamide group attached to a benzene ring, with one of them containing an acetamide end on the opposite side and the other two a cyclopropyl group, in order to increase the solubility of the compounds. However, the biological evaluation of the compounds showed that satisfactory cell death percentage occurs only by administering a high concentration of the drugs to the tested cell lines, demonstrating the need for further investigation, in order to be able to compete with commercially available BRAF inhibitors.
Language Greek, English
Subject Benzohiazole derivatives
Braf inhibitors
Organic synthesis
Αναστολείς του Braf
Βενζοθειαζολικά παράγωγα
Βιοδραστικές ενώσεις
Οργανική σύνθεση
Issue date 2023-12-08
Collection   School/Department--School of Medicine--Department of Medicine--Post-graduate theses
  Type of Work--Post-graduate theses
Permanent Link https://elocus.lib.uoc.gr//dlib/4/c/4/metadata-dlib-1699260284-225377-23826.tkl Bookmark and Share
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