1-aril-2-(4-metilpirazol-1-il) etanon oksim türevlerinin sentezi ve sitotoksik etkilerinin değerlendirilmesi
Küçük Resim Yok
Tarih
2025
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
İnönü Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Amaç: Etkili antikanser bileşikler geliştirmek amacıyla çok kapsamlı araştırmalar yapılmaktadır. Kanser tedavisi üzerine yapılan kimyasal çalışmalarda özellikle azol bileşikleri kullanılmıştır. Azol fonksiyonel grubu içerisinden en çok tercih edilen halka iskeleti ise pirazol halka yapısıdır. Yeni tedavi seçeneklerinde amaç daha az toksik, yan etkileri azaltılmış, hasta için uygulanabilirliği arttırılmış ilaçlar keşfetmektedir. Bu tez çalışmasında "1-(4-Klorofenil)-2-(4-metilpirazol-1-il)etanon oksim" yapısına sahip bileşiklerin tasarlanması, sentezi ve sitotoksik etkilerinin incelenmesi amaçlanmaktadır. Materyal ve Metot: Bu çalışmada 11 yeni bileşiğin tasarlanması, sentezi ve sitotoksik değerlendirilmesi yapılmıştır. Bileşiklerin yapısı 1H-NMR, 13C-NMR ve kütle spektrumu sonucu elde edilen bilgilerle aydınlatılmıştır. Bileşiklerin MCF-7, C6, SH-SY5Y hücre hatlarına karşı in vitro antikanser aktiviteleri ile aydınlatılmıştır. Bulgular: Yapılan antikanser aktivite çalışmaları sonucunda sentezlenen bileşiklerin MCF-7, C6 ve SH-SY5Y hücre hatlarında % canlılık değerleri ve IC50 değerleri hesaplanmıştır. En iyi aktivitenin görüldüğü hücre hattı olan C6 hücre hattında yapı etki ilişkisi ile sonuçların değerlendirilmesi yapılmıştır. Sonuç: Bu denklemler kullanılarak 11 yeni bileşik sentezlenmiştir. G10 bileşiğinin C6 hücre hattına etkili ve aynı zamanda yüksek seçicilik değerine sahip olduğu bulunmuştur. En düşük aktiviteye sahip bileşikler ise G8 ve G9 bileşikleridir. Sentezlenen bileşiklerin hücre canlılığı SH-SY5Y hücre hattına karşı değerlendirilmiştir. Canlı hücreye karşı G10 bileşiğinin diğer bileşiklere göre daha az toksik olduğu yapılan çalışmalarla kanıtlanmıştır. Anahtar Kelimeler: Antikanser, Oksim, Pirazol
Aim: Extensive research is being conducted to develop effective anticancer compounds. Azole compounds, in particular, have been utilized in chemical studies focused on cancer treatment. Among azole functional groups, the pyrazole ring structure is the most frequently preferred scaffold. The goal in new therapeutic options is to discover drugs that are less toxic, have reduced side effects, and offer increased patient applicability. This thesis aims to design, synthesize, and investigate the cytotoxic effects of compounds with the "1-(4-chlorophenyl)-2-(4-methylpyrazol-1-yl)ethanone oxime" structure. Material and method: In this study, 11 new compounds were designed, synthesized, and subjected to cytotoxic evaluation. The structures of the compounds were elucidated using data obtained from 1H-NMR, 13C-NMR, and mass spectrometry. Their in vitro anticancer activities against MCF-7, C6, and SH-SY5Y cell lines were also investigated. Results: As a result of the anticancer activity studies, the percentage viability and IC50 values of the synthesized compounds in MCF-7, C6, and SH-SY5Y cell lines were calculated. The results were evaluated based on structure-activity relationships in the C6 cell line, which showed the best activity. Conclusıon: Using these equations, 11 new compounds were synthesized. Compound G10 was found to be effective against the C6 cell line and also exhibited high selectivity. Compounds G8 and G9 showed the lowest activity. The cell viability of the synthesized compounds was evaluated against the SH-SY5Y cell line. Studies proved that compound G10 is less toxic to living cells compared to the other compounds. Keywords: Anticancer, Oxime, Pyrazole
Aim: Extensive research is being conducted to develop effective anticancer compounds. Azole compounds, in particular, have been utilized in chemical studies focused on cancer treatment. Among azole functional groups, the pyrazole ring structure is the most frequently preferred scaffold. The goal in new therapeutic options is to discover drugs that are less toxic, have reduced side effects, and offer increased patient applicability. This thesis aims to design, synthesize, and investigate the cytotoxic effects of compounds with the "1-(4-chlorophenyl)-2-(4-methylpyrazol-1-yl)ethanone oxime" structure. Material and method: In this study, 11 new compounds were designed, synthesized, and subjected to cytotoxic evaluation. The structures of the compounds were elucidated using data obtained from 1H-NMR, 13C-NMR, and mass spectrometry. Their in vitro anticancer activities against MCF-7, C6, and SH-SY5Y cell lines were also investigated. Results: As a result of the anticancer activity studies, the percentage viability and IC50 values of the synthesized compounds in MCF-7, C6, and SH-SY5Y cell lines were calculated. The results were evaluated based on structure-activity relationships in the C6 cell line, which showed the best activity. Conclusıon: Using these equations, 11 new compounds were synthesized. Compound G10 was found to be effective against the C6 cell line and also exhibited high selectivity. Compounds G8 and G9 showed the lowest activity. The cell viability of the synthesized compounds was evaluated against the SH-SY5Y cell line. Studies proved that compound G10 is less toxic to living cells compared to the other compounds. Keywords: Anticancer, Oxime, Pyrazole
Açıklama
Anahtar Kelimeler
Eczacılık ve Farmakoloji, Pharmacy and Pharmacology
