Synthesis and in vitro antitumor activities of novel thioamide substituted piperazinyl-1,2,4-triazines

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dc.authorid0000-0002-5976-676X
dc.authorid0000-0003-1896-2729
dc.authorid0000-0001-6047-2796
dc.authorid0000-0002-0841-1299
dc.contributor.authorŞahin, Zafer
dc.contributor.authorBiltekin, Sevde Nur
dc.contributor.authorOzansoy, Mehmet
dc.contributor.authorHemiş, Bervis
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorBerk, Barkın
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2022-12-06T07:33:00Z
dc.date.available2022-12-06T07:33:00Z
dc.date.issued2022
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.abstractTriazines are in great interest for their potential to mimic nucleoside analog compounds. Three different isomers exist including 1,2,3-triazine, 1,3,5-triazine (s-triazine) and 1,2,4-triazine. All of these skeletons were investigated. Among them, 5,6-diaryltriazines were previously tested on MCF7 and other tumor cell lines. In this study, we have synthesized and characterized 9 novel 5,6-diaryl-1,2,4-triazine derivatives (4a-i) using (HNMR)-H-1, (CNMR)-C-13, and HRMS spectra. Contributing to the previous data, we tested our compounds on U87MG, C6 and SH-SY5Y cell lines along with MCF7. We evaluated if these compounds affect CNS tumors in vitro, which cell lines have different protein profiles from MCF7 and mainly nucleosides are used as their antiproliferative agents. Briefly, compounds showed good antitumor activity on the C6 cell line with up to 50% inhibition for 7 of 9 compounds (4b, 4d-i) at 50 mu M. Additionally, compounds showed moderate activity on U87MG glioblastomas, compound 4a was the most active with 29.68 mu M IC50. Compounds did not show significant activity on SH-SY5Y cells. Cytotoxicity evaluation gave the results that the synthesized compounds show moderate cytotoxicity on NIH-3T3 and severe cytotoxicity on HEK 293. The study leads the investigations of triazines with glioma cell lines.
dc.identifier.citationŞahin, Z., Biltekin, S. N., Ozansoy, M., Hemiş, B., Yurttaş, L., Berk, B. ... Demirayak, Ş. (2022). Synthesis and in vitro antitumor activities of novel thioamide substituted piperazinyl-1,2,4-triazines. Journal of Heterocyclic Chemistry, 59(8), 1333-1340. https://doi.org/10.1002/jhet.4470
dc.identifier.doi10.1002/jhet.4470
dc.identifier.endpage1340
dc.identifier.issn0022-152X
dc.identifier.issn1943-5193
dc.identifier.issue8
dc.identifier.scopus2-s2.0-85125675499
dc.identifier.scopusqualityQ3
dc.identifier.startpage1333
dc.identifier.urihttps://doi.org/10.1002/jhet.4470
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10078
dc.identifier.volume59
dc.identifier.wos000765052900001en_US
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorŞahin, Zafer
dc.institutionauthorBiltekin, Sevde Nur
dc.institutionauthorBerk, Barkın
dc.institutionauthorDemirayak, Şeref
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofJournal of Heterocyclic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectPiperazinyl-1,2,4-Triazines
dc.subjectThioamide
dc.subjectAntitumor Activities
dc.titleSynthesis and in vitro antitumor activities of novel thioamide substituted piperazinyl-1,2,4-triazines
dc.typeArticle

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