Synthesis and antitumor activity evaluation of new 2-(4-aminophenyl)benzothiazole derivatives bearing different heterocyclic rings

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dc.contributor.authorYurttaş, Leyla
dc.contributor.authorTay, Funda
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned10.07.201910:49:13
dc.date.accessioned2019-07-10T19:58:04Z
dc.date.available10.07.201910:49:13
dc.date.available2019-07-10T19:58:04Z
dc.date.issued2015
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.descriptionWOS: 000359815200017
dc.descriptionPubMed ID: 25198890
dc.description.abstractTwenty-five new N-[4-(benzothiazole-2-yl)phenyl]acetamide derivatives bearing different heterocyclic ring systems were synthesized using 2-(4-aminophenyl)benzothiazole structure as a pharmacophoric group. Final compounds were screened for their potential antitumor activity in vitro against approximately 60 human tumor cell lines derived from nine neoplastic diseases at National Cancer Institute, USA. 2-(4-Aminophenyl)benzothiazole structure was prepared by the reaction of 4-aminobenzoic acid and 2-aminothiophenol in polyphosphoric acid using microwave irradiation. After acetylation reaction, amide compounds 2a and 2b were obtained, which were then reacted with 2-mercapto(benz)imidazole/benzothiazole/benzoxazole derivatives in acetone with the presence of potassium carbonate to gain final compounds (3-27). Among all tested compounds, compound 10, namely N-[4-(benzothiazole-2-yl)-3-chlorophenyl]-2-[(benzimidazole-2-yl)thio]acetamide, and compound 16, namely N-[4(benzothiazole-2-yl)phenyl]-2-[(1,5-diphenyl-1H-imidazole-2-yl)thio]acetamide, were found to be of considerable anticancer activity against some cancer cell lines.
dc.description.sponsorshipCommission of Scientific Research Projects of Eskisehir Osmangazi University [ESOGU/200819010]; Eskisehir Osmangazi Universityen_US
dc.description.sponsorshipThis work was supported by the Commission of Scientific Research Projects of Eskisehir Osmangazi University (ESOGU/200819010). The authors gratefully acknowledge the financial support by Eskisehir Osmangazi University.en_US
dc.identifier.citationYurttaş, L., Tay, F. ve Demirayak, Ş. (2015). Synthesis and antitumor activity evaluation of new 2-(4-aminophenyl)benzothiazole derivatives bearing different heterocyclic rings. Journal of Enzyme Inhibition and Medicinal Chemistry, 30(3), 458-465. https://dx.doi.org/10.3109/14756366.2014.945168
dc.identifier.doi10.3109/14756366.2014.945168
dc.identifier.endpage465
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue3
dc.identifier.scopusqualityQ1
dc.identifier.startpage458
dc.identifier.urihttps://dx.doi.org/10.3109/14756366.2014.945168
dc.identifier.urihttps://hdl.handle.net/20.500.12511/3102
dc.identifier.volume30
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherTaylor & Francis
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subject2-(4-Aminophenyl)Benzothiazole
dc.subjectAnticancer Activity
dc.subjectAntitumor Activity
dc.subjectSynthesis
dc.titleSynthesis and antitumor activity evaluation of new 2-(4-aminophenyl)benzothiazole derivatives bearing different heterocyclic rings
dc.typeArticle

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