Potent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives

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dc.authorid0000-0002-2289-7950
dc.authorid0000-0002-5976-676X
dc.authorid0000-0001-6047-2796
dc.contributor.authorErtaş, Merve
dc.contributor.authorŞahin, Zafer
dc.contributor.authorBülbül, Emre Fatih
dc.contributor.authorBender, Ceysu
dc.contributor.authorBiltekin, Sevde Nur
dc.contributor.authorBerk, Barkın
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorNalbur, Aysu M.
dc.contributor.authorÇelik, Hayati
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2019-12-26T08:52:52Z
dc.date.available2019-12-26T08:52:52Z
dc.date.issued2019
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı
dc.description.abstractThe antioxidant, antimalarial, antibacterial, and antitumor activities of thiosemicarbazones have made this class of compounds important for medicinal chemists. In addition, thiosemicarbazones are among the most potent and well-known ribonucleotide reductase inhibitors. In this study, 24 new thiosemicarbazone derivatives were synthesized, and the structures and purity of the compounds were determined by IR, H-1 NMR, C-13 NMR, mass spectroscopy, and elemental analysis. The IC50 values of these 24 compounds were determined with an assay for ribonucleotide reductase inhibition. Compounds 19, 20, and 24 inhibited ribonucleotide reductase enzyme activity at a higher level than metisazone as standard. The cytotoxic effects of these compounds were measured on the MCF7 (human breast adenocarcinoma) and HEK293 (human embryonic kidney) cell lines. Similarly, compounds 19, 20, and 24 had a selective effect on the MCF7 and HEK293 cell lines, killing more cancer cells than cisplatin as standard. The compounds (especially 19, 20, and 24 as the most active ones) were then subjected to docking experiments to identify the probable interactions between the ligands and the enzyme active site. The complex formation was shown qualitatively. The ADME (absorption, distribution, metabolism, and excretion) properties of the compounds were analyzed using in-silico techniques.
dc.identifier.citationErtaş, M., Şahin, Z., Bülbül, E. F., Bender, C., Biltekin, S. N., Berk, B. ... Demirayak, Ş. (2019). Potent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives. Archiv der Pharmazie, 352(11). https://doi.org/10.1002/ardp.201900033
dc.identifier.doi10.1002/ardp.201900033
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue11
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1002/ardp.201900033
dc.identifier.urihttps://hdl.handle.net/20.500.12511/4719
dc.identifier.volume352
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofArchiv der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectAntitumor Agents
dc.subjectRibonucleotide Reductase
dc.subjectThiazole
dc.subjectThiosemicarbazone
dc.titlePotent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives
dc.typeArticle

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