Antiproliferative properties of 2'-alkoxymethyl substituted klavuzon derivatives
tarafından
Yıldız, Mehmet Salih, author.
Başlık
:
Antiproliferative properties of 2'-alkoxymethyl substituted klavuzon derivatives
Yazar
:
Yıldız, Mehmet Salih, author.
Yazar Ek Girişi
:
Yıldız, Mehmet Salih, author.
Fiziksel Tanımlama
:
xi, 52 leaves:+ 1 computer laser optical disc.
Özet
:
One of the main objectives of studies on anticancer agents is that the agent is expected to show a high cytotoxic activity on cancer cells and show a less cytotoxic effect on the contrary in healthy cells or never show cytotoxic activity. (R)- goniothalamin, isolated from the Goniothalamus plant, is a styryl lactone and has been found to have a selective antiproliferative property on cancer cells in studies conducted. The Michael acceptor feature in the structure of goniothalamin is thought to be covalently bonded to the nucleophilic side chains of the enzymes and show activity in this way. In previous studies, it has been shown that 1-naphthyl substituted 5,6-dihydro- 2H-pyran-2-one derivatives and 4'-methyl klavuzon derivatives exhibit higher cytotoxic activity on cancer cells than goniothalamin. In this study, antiproliferative properties of newly synthesized 2'-alkoxymethyl substituted klavuzon derivatives have been examined and MIA PaCa-2 pancreatic cancer cell lines and HPDEC pancreatic healthy cell lines were used. MTT cell viability tests were performed at the first step of this study. As a result of this study, it has been observed that the 2'-isobutoxymethylklavuzon derivative has selective cytotoxic activity on the MIA PaCa-2 cell line. It showed activity at lower concentrations than goniothalamin. Cytotoxic activities of the compounds are associated with the size of the R group at position 2’-. Methoxymethyl substituted the worst selective activity among these compounds whereas isobutoxy derivative the best selective one. In the second stage of the study, the inhibition on topoisomerase I enzyme was studied. The 2'-alkoxymethyl klavuzon derivatives were found to have Topo I enzyme inhibition properties depending on concentration and time manner. The study continued with choices methoxy and isobutoxy derivatives and these two compounds caused an arrest at G1 phase and DNA damage. Also, isobutoxy derivative induced apoptosis in the MIA PaCa-2 pancreatic cancer cell lines.
Konu Başlığı
:
Cell cycle.
Apoptosis.
Antineoplastic agents.
Yazar Ek Girişi
:
Çağır, Ali,
Tüzel Kişi Ek Girişi
:
İzmir Institute of Technology. Biotechnology.
Tek Biçim Eser Adı
:
Thesis (Master)--İzmir Institute of Technology: Biotechnology.
İzmir Institute of Technology: Biotechnology--Thesis(Master).
Elektronik Erişim
:
Library | Materyal Türü | Demirbaş Numarası | Yer Numarası | Durumu/İade Tarihi |
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IYTE Library | Tez | T001620 | QH605 .Y514 2017 | Tez Koleksiyonu |