A master thesis from Aalborg University
SYNTHESIS OF ANTICANCER PRODRUGS FOR ENHANCED COMPLEXATION WITH CYCLODEXTRIN
[Syntese af anticancer prodrugs for forbedret kompleksdannelse med cyclodextrin]
Author(s)
Term
4. term
Education
Publication year
2017
Submitted on
2017-06-09
Pages
215 pages
Abstract
Kræft anslås at være ansvarlig for 13 % af alle dødsfald på verdensplan i 2012. Den primære behandling for kræft er fortsat kemoterapi, men behandlingen er langt fra perfekt. Kemoterapi kæmper blandt andet med problemer som lav specificitet og systemisk toksicitet. En måde at forbedre kemoterapi er ved hjælp af såkaldte nanocarriers, så som cyclodextriner. Dette studie beskæftiger sig med syntesen af prodrugs fra kendte anti-kræft medicin for at øge deres kompleksdannelse med cyclodextriner. Fokus har været på syntesen af Doxorubicin og Gemcitabin prodrugs for at minimere bivirkningerne og forbedre deres affinitet. Det blev vurderet hvilke linker, der ville virke bedst for hvert molekyle. I alt blev fire prodrugs (to af hver) syntetiseret. Hver af de endelige produkter blev isoleret i ~10-20 mg. Kompleksdannelsen af de syntetiseret prodrugs blev analyseret via ITC. Fem forskellige β-cyclodextrin derivater blev udvalgt og de opnåede KA værdierne blev sammenlignet.
Cancer was responsible for an estimated 13% of all deaths worldwide in 2012. The main treatment for cancer remains chemotherapy; however, it faces problems due to low specificity and systemic toxicity. A way to improve chemotherapy is to use nanocarriers such as cyclodextrins. This study concerns the synthesis of prodrugs from known anticancer drugs to enhance their complexation with cyclodextrins. The focus has been on the synthesis of Doxorubicin and Gemcitabine prodrugs in order to improve their complexation with cyclodextrin and thereby minimize the side effects and improve their affinity. Assessments of each molecule were made and four different prodrugs (two of each) were designed and synthesized. The final four products were isolated in ~10-20 mg. The complex formation of the synthesized prodrugs was analyzed by ITC. Five different β-cyclodextrins derivatives were chosen and obtained KA values were compared.
Documents
Colophon: This page is part of the AAU Student Projects portal, which is run by Aalborg University. Here, you can find and download publicly available bachelor's theses and master's projects from across the university dating from 2008 onwards. Student projects from before 2008 are available in printed form at Aalborg University Library.
If you have any questions about AAU Student Projects or the research registration, dissemination and analysis at Aalborg University, please feel free to contact the VBN team. You can also find more information in the AAU Student Projects FAQs.