Ag- n-heterosiklik karben komplekslerinin antitümör aktivitesinin incelenmesi
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Dosyalar
Tarih
2017
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
İnönü Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/embargoedAccess
Özet
N-Heterosiklik karbenler (NHC) son yıllarda büyük ilgi gören, kuvvetli nükleofil özelliğine sahip ve geçiĢ metallerine kararlı bağlanabilen ligant sınıfıdır. Genellikle katalitik uygulamalarda kullanılan bu ligantlar son yıllarda biyolojik aktiviteler göstermelerinden dolayı klinik uygulamalarda da kullanılmaya baĢlanmıĢtır. Günümüzde metal NHC komplekslerinin en aktif olduğu alanlardan biri biyoorganometalik kimyadır. Kanser ve enfeksiyon hastalıklarının tedavisinde kullanılan metal bazlı ilaçların gelişimi önemli bir alan oluşturmaktadır ki çoğu metal NHC kompleksleriyle bu alanda çalışılmaktadır. N-Heterosiklik karbenlerin metallerle yapmıĢ oldukları bağların yüksek stabilite göstermesi ve türevlendirilmesinin kolay olması karbenleri ilaç geliştirme için uygun bir aday yapmaktadır. Son zamanlarda antimikrobiyal ve daha yakın zamanda antitümör ajanları olarak tedavi edici araĢtırmalarda NHC metal komplekslerinin kullanımı artmıĢtır Bu nedenle tez kapmasında yeni Ag-N-heterosiklik karben kompleksleri sentezlenmiĢ ve antitümör aktiviteleri incelenmiĢtir. Bulunan sonuçlar üç başlıkta özetlenebilir 1) Tezde 1,3-dialkilbenzimidazolyum (1a-c), propil-3-sülfonatbenzimidazolyum (2a-b) ve bütil-4-sülfonatbenzimidazolyum (3) tuzları sentezlenmiş, yapıları uygun spektroskopik yöntemlerle aydınlatılmıştır. 2) Benzimidazolyum tuzları Ag2O ile etkileştirilerek Ag(I)-benzimidazol-2-iliden (4a-c), propil-3-sülfonatbenzimidazol-2-iliden (5) ve bütil-4-sülfonatbenzimidazol-2-iliden gümüş(I) (6) kompleksleri hazırlanmıştır ve yapıları uygun spektroskopik yöntemlerle aydınlatılmıştır. 3) Elde edilen Ag-NHC komplekslerinin antitümör aktiviteleri incelenmiştir. Sentezlenen bu komplekslerinin doz (15-100 µM) ve güne (1-3 gün) bağlı olarak sağlıklı fibroblast hücre hattı (L-929), karaciğer kanseri hücre hattı (Hep3B) ve beyin kanseri hücre hattındaki (SH-SY5Y) antitümör aktiviteleri MTS sitotoksisite testi ile belirlenmiştir.
N-Heterocyclic carbenes (NHC) are of great interest in recent years, and have a strong nucleophilic character and are capable of stable binding to transition metals. These ligands, which are generally used in catalytic applications, have begun to be used in clinical applications due to their biological activity in recent years. One of the areas where metal NHC complexes are most active today is bioorganometallic chemistry. The development of metal-based drugs used in the treatment of cancer and infectious diseases constitutes an important area in which many metal NHC complexes work in this area. N-Heterocyclic carbenes have high stability in the ligands they have made with metals, and their easy derivatization makes carbides a suitable candidate for drug development. Recently, the use of NHC metal complexes has been increased in antimicrobial and more recently as therapeutic antitumor agents. Therefore, new Ag-N-heterocyclic carbene complexes have been synthesized and antitumor activities have been investigated. The results of this study could be summarized in three main sections: 1) In the first part, 1,3-dialkylbenzimidazolium(1a-c), propil-3-sulphonate benzimidazolium (2a-b) and buthyl-4-sulphonatebenzimidazolium(3) salts were synthesized and their structure were elucidated spectroscopic techniques. 2) In the second part, benzimidazol-2-ylidene (4a-c), propyl-3-sulphonatebenzimidazol-2-ylidene (5) and butyl-4sulphonate benzimidazol-2-ylidene silver(I) (6) complexes were synthesized from reaction of Ag2O with benzimidazolium salts, and all complexes were structurally elucidated by means of spectroscopy. 3) The antitumor activities of the obtained Ag-NHC complexes were investigated. Antitumor activities of these complexes were determined by MTS cytotoxicity test in healthy fibroblast cell line (L-929), liver cancer cell line (Hep3B) and brain cancer cell line (SH-SY5Y) depending on dose (15-100 μM) and sun (1-3 days).
N-Heterocyclic carbenes (NHC) are of great interest in recent years, and have a strong nucleophilic character and are capable of stable binding to transition metals. These ligands, which are generally used in catalytic applications, have begun to be used in clinical applications due to their biological activity in recent years. One of the areas where metal NHC complexes are most active today is bioorganometallic chemistry. The development of metal-based drugs used in the treatment of cancer and infectious diseases constitutes an important area in which many metal NHC complexes work in this area. N-Heterocyclic carbenes have high stability in the ligands they have made with metals, and their easy derivatization makes carbides a suitable candidate for drug development. Recently, the use of NHC metal complexes has been increased in antimicrobial and more recently as therapeutic antitumor agents. Therefore, new Ag-N-heterocyclic carbene complexes have been synthesized and antitumor activities have been investigated. The results of this study could be summarized in three main sections: 1) In the first part, 1,3-dialkylbenzimidazolium(1a-c), propil-3-sulphonate benzimidazolium (2a-b) and buthyl-4-sulphonatebenzimidazolium(3) salts were synthesized and their structure were elucidated spectroscopic techniques. 2) In the second part, benzimidazol-2-ylidene (4a-c), propyl-3-sulphonatebenzimidazol-2-ylidene (5) and butyl-4sulphonate benzimidazol-2-ylidene silver(I) (6) complexes were synthesized from reaction of Ag2O with benzimidazolium salts, and all complexes were structurally elucidated by means of spectroscopy. 3) The antitumor activities of the obtained Ag-NHC complexes were investigated. Antitumor activities of these complexes were determined by MTS cytotoxicity test in healthy fibroblast cell line (L-929), liver cancer cell line (Hep3B) and brain cancer cell line (SH-SY5Y) depending on dose (15-100 μM) and sun (1-3 days).
Açıklama
Anahtar Kelimeler
Biyokimya, Biochemistry
Kaynak
WoS Q Değeri
Scopus Q Değeri
Cilt
Sayı
Künye
Kızrak, Ü. (2017). Ag- n-heterosiklik karben komplekslerinin antitümör aktivitesinin incelenmesi. İnönü Üniversitesi. Malatya.
