Formulation, characterization, cytotoxicity and Salmonella/microsome mutagenicity (Ames) studies of a novel 5-fluorouracil derivative

Simple item page
dc.contributor.authorKöksal Karayildirim Ç.
dc.contributor.authorKotmakçi M.
dc.contributor.authorHalay E.
dc.contributor.authorAy K.
dc.contributor.authorBaşpinar Y.
dc.date.accessioned2024-07-22T08:10:03Z
dc.date.available2024-07-22T08:10:03Z
dc.date.issued2018
dc.description.abstract5-Fluorouracil is one of the first line drugs for the systemic therapy of solid tumors like breast, colorectal, oesophageal, stomach, pancreatic, head and neck. It could be shown that sugars can improve the absorption across cell membranes and can help to bypass some pharmacokinetic problems. Carbohydrates as most common organic molecules are an important issue of plant and animal metabolisms. They are non toxic and have important duties in the body like participating in DNA and RNA synthesis and being responsible for energy production. In addition, they have many hydroxyl, aldehyde and ketone groups that attract attention for synthesis as a potential drug derivative. 1,2,3,-Triazole compounds have also important role in heterocyclic chemistry because of their pharmaceutical properties and their high reactivity, which could be used as a building block for complex chemical compounds. In this study, following the “Click Reaction” of 5-FU and tetra-O-acetylglycose the 5-fluorouracil derivative 1-[{1′-(2″,3″,4″,6″-tetra-O-acetyl-β-D-glycopyronosyl)-1′H-1′,2′,3′-triazole-4′-yl} methyl]5-fluorouracil was synthesized. Following, a micellar formulation of 5-Fluorouracil derivative was prepared and characterized in terms of particle size, polydispersity index, zeta potential, refractive index and pH. Furthermore, the cytotoxicity and mutagenicity of the 5-fluorouracil derivative was investigated using an in vitro cell culture model and the AMES test. According to the results of this study, the novel 5-fluorouracil derivative could be a drug candidate for the therapy of cancer and needs further in vivo investigations. © 2018 The Authors
dc.identifier.DOI-ID10.1016/j.jsps.2018.01.004
dc.identifier.issn13190164
dc.identifier.urihttp://akademikarsiv.cbu.edu.tr:4000/handle/123456789/15070
dc.language.isoEnglish
dc.publisherElsevier B.V.
dc.rightsAll Open Access; Gold Open Access; Green Open Access
dc.subject1 [[1' (2'',3'',4,'',6'' tetra o acetyl beta dextro glycopyranosyl) 1'h 1',2',3' triazole 4' yl]methyl] 5 fluorouracil
dc.subjectfluorouracil derivative
dc.subjectunclassified drug
dc.subjectAmes test
dc.subjectantineoplastic activity
dc.subjectArticle
dc.subjectclick chemistry
dc.subjectcontrolled study
dc.subjectcytotoxicity
dc.subjectdispersity
dc.subjectdrug formulation
dc.subjectdrug synthesis
dc.subjecthuman
dc.subjecthuman cell
dc.subjectin vitro study
dc.subjectmicelle
dc.subjectmutagenicity
dc.subjectparticle size
dc.subjectpH
dc.subjectrefraction index
dc.subjectzeta potential
dc.titleFormulation, characterization, cytotoxicity and Salmonella/microsome mutagenicity (Ames) studies of a novel 5-fluorouracil derivative
dc.typeArticle

Files

Collections

Scopus Koleksiyonu