Synthesis of new imine-/amine-bearing imidazo[1,2-a]pyrimidine derivatives and screening of their cytotoxic activity

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dc.authoridAtalay, Hazal Nazlican/0000-0001-8859-0268
dc.contributor.authorGungor, Tugba
dc.contributor.authorAtalay, Hazal Nazlican
dc.contributor.authorYilmaz, Yakup Berkay
dc.contributor.authorTumer, Tugba Boyunegmez
dc.contributor.authorAy, Mehmet
dc.date.accessioned2025-01-27T20:49:34Z
dc.date.available2025-01-27T20:49:34Z
dc.date.issued2023
dc.departmentÇanakkale Onsekiz Mart Üniversitesi
dc.description.abstractImidazo[1,2-a]pyrimidine derivatives bearing imine groups (3a-e) were successfully synthesized in moderate to good yields using microwave-assisted heating. Corresponding amine derivatives (4a-e) were also obtained by the reduction reaction of the imine derivatives (3a-e). All synthesized products were characterized by FT-IR,1H NMR, 13C NMR, and LC-MS spectroscopic techniques. In silico ADMET, Lipinski, and drug-likeness studies of the compounds were conducted and all were found to be suitable drug candidates. The cytotoxicity of the potential drug molecules was screened against the breast cancer cell lines MCF-7 and MDA-MB-231 and the healthy model HUVEC by the sulforhodamine B method. According to the antiproliferative studies, compounds 3d and 4d showed remarkable inhibition of MCF-7 cells with IC50 values of 43.4 and 39.0 mu M and of MDA-MB-231 cells with IC50 values of 35.9 and 35.1 mu M, respectively. In particular, compound 3d selectively inhibited the proliferation of MCF-7 1.6-fold and MDA-MB-231 2.0-fold relative to healthy cells. Moreover, the apoptotic mechanism studies indicated that compound 4d induced apoptosis by moderately increasing the ratio of Bax/Bcl-2 genes. Imidazo[1,2-a]pyrimidine derivative 3d, a promising cytotoxic agent, may be helpful in the discovery of new and more efficient anticancer agents for breast cancer treatment.
dc.description.sponsorshipCanakkale Onsekiz Mart University [FBA-2020-3439]
dc.description.sponsorshipThis study was financially supported by a research grant from Canakkale Onsekiz Mart University, Scientific Research Projects, ID: FBA-2020-3439.
dc.identifier.doi10.55730/1300-0527.3594
dc.identifier.endpage+
dc.identifier.issn1300-0527
dc.identifier.issue5
dc.identifier.pmid38173738
dc.identifier.scopus2-s2.0-85176107626
dc.identifier.scopusqualityQ3
dc.identifier.startpage1064
dc.identifier.trdizinid1208422
dc.identifier.urihttps://doi.org/10.55730/1300-0527.3594
dc.identifier.urihttps://search.trdizin.gov.tr/tr/yayin/detay/1208422
dc.identifier.urihttps://hdl.handle.net/20.500.12428/25223
dc.identifier.volume47
dc.identifier.wosWOS:001099801900013
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakTR-Dizin
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherTubitak Scientific & Technological Research Council Turkey
dc.relation.ispartofTurkish Journal of Chemistry
dc.relation.publicationcategoryinfo:eu-repo/semantics/openAccess
dc.rightsinfo:eu-repo/semantics/openAccess
dc.snmzKA_WoS_20250125
dc.subjectBreast cancer
dc.subjectcytotoxicity
dc.subjectimidazo[1,2-a]pyrimidine
dc.subjectimine
dc.subjectmicrowave
dc.titleSynthesis of new imine-/amine-bearing imidazo[1,2-a]pyrimidine derivatives and screening of their cytotoxic activity
dc.typeArticle

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