Evaluation of anticancer and aromatase inhibition activity of newly synthesized thiazoles
2015
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Advisor: Yrd. Doç. Dr. Leyla Yurttaş ; Prof. Dr. Şeref Demirayak
Abstract (EN)
Breast cancer is a cancer type which has been treating by inhibiting of estrogen synthesis in human body, and commonly seen in women. Aromatase, can be thought from its name, provides an aromatic ring to a non-aromatic cycle, so that the estrogen. Caused by important side effect feedbacks about steroid inhibitors which was used as primary agents in breast cancer, an alternative treatment is required. For this reason, non-steroidal inhibitors of aromatase developed consist a thiazole ring with aromatic functional groups on both sides. Additionally, as aromatase is a cyp 450 enzyme, includes a haem group and iron. Complexion by this iron group by a specific function group can provide specific activity. For the optimization of drug metabolism and obtaining best activity, functional groups on both sides of thiazole have considerable importance. In our study, 2-pyridyl -4-phenolesubstituted thiazole derivatives which are synthesized for this aim, have been evaluated for their anticancer activity by XTT assay. Compounds were synthesized by Hantzsch method and physical analysis and structural determination studies were performed. Reaction yields showed compatibility with literature and spectral studies verified the structure of compounds compared expectations. Among the synthesized compounds, compound 7 (showed best anticancer activity with the XTT method by its IC50 value. Furthermore, results of molecular modelling results showed convenience to biological evaluation.
Author
Zafer Şahin
How to Cite
Zafer Şahin (Master Thesis). Evaluation of anticancer and aromatase inhibition activity of newly synthesized thiazoles, 2015, Anadolu University.
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