Investigation of metal based phenyl-functionalized pyridyl-triazolylidenes for their antitumor activity in vitro

Gržan, Tena (2016) Investigation of metal based phenyl-functionalized pyridyl-triazolylidenes for their antitumor activity in vitro. Diploma thesis, Faculty of Science > Department of Biology.

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Abstract

Although there has been a great progress in elucidating the mechanisms of malignant diseases and the improvement in diagnostic methods, cancers remain one of the biggest health problem today. One of the cancer therapies is chemotherapy. However, despite its success in treating certain types of cancer, the resistance and the unwanted side effects are still representing the greatest challenges to this treatment. In order to reduce or overcome the above disadvantages there is a continuous need to synthesize new compounds. Organometallic complexes based on different metals and ligands have already showed anticancer activities. This research investigated the cytotoxic activity of twelve compounds: [(arene)M(phenyl-functionalized pyridyl-1,2,3-triazol-5-ylidene)chlor] (M = iridium, osmium or ruthenium, arene = 1,2,3,4,5- pentamethylcyclopentadienyl or p-cymen) in human cervix carcinoma cell line (HeLa) using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays. Iridium(III) compound ABB43 showed higher cytotoxicity, even than cisplatin, the widely used cytostatic. ABB43 cytotoxicity was investigated in several other tumor cell lines and normal cell line. Higher cytotoxicity levels in tumor cell lines in regard to normal cell line indicate the potential use of the complex as anticancer drug. It was showen by flow cytometry that ABB43 blocks the S/G2 phase of the cell cycle and induces apoptosis. Specific inhibitors or stimulators of the synthesis of cellular glutathione (GSH) have showed that GSH plays a role in the cell response to stress caused by ABB43 treatment.

Item Type: Thesis (Diploma thesis)
Keywords: organometallic complexes, drug resistance, iridium, glutathione
Supervisor: Brozović, Anamaria
Co-supervisor: Matulić, Maja
Date: 2016
Number of Pages: 41
Subjects: NATURAL SCIENCES > Biology
Divisions: Faculty of Science > Department of Biology
Depositing User: Silvana Šehić
Date Deposited: 25 Mar 2016 08:25
Last Modified: 25 Mar 2016 08:25
URI: http://digre.pmf.unizg.hr/id/eprint/4646

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