Yazar "Dönmez, Serhat" seçeneğine göre listele

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  • Küçük Resim
    Öğe
    Elucidating the anticancer activities of novel triarylbenzophenone derivatives by mechanism-based and in silico approaches
    (Çanakkale Onsekiz Mart Üniversitesi, 2023) Dönmez, Serhat; Tümer, Tuğba; Özbil, Mehmet
    Son zamanlarda çok hedefli ilaçların geliştirilmesi kanser tedavisinde kullanılan stratejilerden biridir. Bu strateji, ilaçların etki gücünü arttırmakla beraber istenmeyen yan etkileri de azaltmaktadır. Bu çalışmada, özgün triarilbenzofenon türevlerinin antikanser aktiviteleri ve dual (ikili) topoizomeraz I/II inhibisyon kapasitelerini in vitro ve in silico teknikleri kullanarak araştırılmıştır. Bulgulara göre, özellikle SMR-36 bileşiği prostat ve kolon kanseri hücrelerinin hücre canlılığını, göç ve koloni oluşturma kabiliyetlerini seçici olarak inhibe ederken sağlıklı hücreler üzerinde minimum sitotoksik etkinlik göstermiştir. Ayrıca, triarilbenzofenon türevleri hem topoizomeraz I hem de topoizomeraz II enzim aktivitesini yüksek bir etkinlikle inhibe etmiştir. Enzim inhibisyon deneylerinden elde edilen bulgularla benzer şekilde in siliko moleküler kenetlenme ve dinamik simülasyonları çalışmalarında da bileşiklerin topoizomerazların katalitik bölgesine karşı yüksek bağlanma afinitesi gösterdiği yönünde bulgular elde edilmiştir. Sonuç olarak, triarilbenzofenon türevlerinin ikili topoizomeraz inhibitörleri olarak kanser tedavisinde kullanılmak üzere umut vadeden bir potansiyeline sahip olabilir ve bu bileşikler etkinlikleri arttırılacak şekilde geliştirilebilir.
  • Küçük Resim
    Öğe
    Looking at NSAIDs from a historical perspective and their current status in drug repurposing for cancer treatment and prevention
    (Springer Science and Business Media Deutschland GmbH, 2023) Özleyen, Adem; Yılmaz, Yakup Berkay; Dönmez, Serhat; Atalay, Hazal Nazlıcan; Antika, Gizem; Boyuneğmez Tümer, Tuğba
    Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently prescribed drug classes with wide therapeutic applications over the centuries. Starting from the use of salicylate-containing willow leaves to the recent rise and fall of highly selective cyclooxygenase-2 (COX-2) inhibitors and the latest dual-acting anti-inflammatory molecules, they have displayed a rapid and ongoing evolution. Despite the enormous advances in the last twenty years, investigators are still in search of the design and development of more potent and safer therapy against inflammatory conditions. This challenge has been increasingly attractive as the emergence of inflammation as a common seed and unifying mechanism for most chronic diseases. Indeed, this fact put the NSAIDs in the spotlight for repurposing against inflammation-related disorders. This review attempts to present a historical perspective on the evolution of NSAIDs, regarding their COX-dependent/independent mode of actions, structural and mechanism-based classifications, and adverse effects. Additionally, a systematic review of previous studies was carried out to show the current situation in drug repurposing, particularly in cancers associated with the GI tract such as gastric and colorectal carcinoma. In the case of non-GI-related cancers, preclinical studies elucidating the effects and modes of action were collected and summarized.
  • Küçük Resim
    Öğe
    Synthesis of Selagibenzophenone A and Its Derivatives for Evaluation of Their Antiproliferative, ROR gamma Inverse Agonistic, and Antimicrobial Effect
    (John Wiley and Sons Inc, 2023) Lapinskaite, Ringaile; Atalay, Hazal Nazlıcan; Malatinec, Stefan; Dönmez, Serhat; Çınar, Zeynep Özlem; Schwarz, Patrik F. F.; Perhal, Alexander F. F.; Tümer Boyuneğmez, Tuğba
    We report a modular synthetic approach towards novel derivatives of the naturally occurring arylated benzophenone selagibenzophenone A. The initial strategy for the construction of the carbon framework of the derivatives relied on the Suzuki reaction of 2,4,6-tribromobenzonitrile, and the addition of the aryl lithium species to nitrile to generate imine. However, the formed imines showed remarkable stability toward hydrolysis. Therefore, Suzuki cross-coupling was carried out with 2,4,6-tribromobenzaldehyde and the subsequent addition of organometallic species to the aldehyde. Oxidation of the resulting alcohol ensured the access to desired ketones. The importance of the developed modular strategy is underlined by the discovery of several derivatives with selective cytotoxic effects and potential anti-inflammatory activity superior to the effect of the natural product.