Cytotoxicity effects and biochemical investigation of novel tetrakis-phthalocyanines bearing 2-thiocytosine moieties with molecular docking studies

Basit Öğe Kaydı
dc.authoridParham Taslimi / 0000-0002-3171-0633en_US
dc.authorscopusidParham Taslimi / 56658628800
dc.authorwosidParham Taslimi / AAL-2788-2020
dc.contributor.authorGünsel, Armağan
dc.contributor.authorYıldırım, Aslı
dc.contributor.authorTaslimi, Parham
dc.contributor.authorErden, Yavuz
dc.contributor.authorTaşkın-Tok, Tuğba
dc.date.accessioned2022-02-07T08:28:21Z
dc.date.available2022-02-07T08:28:21Z
dc.date.issued2022en_US
dc.departmentİstinye Üniversitesi, Mühendislik ve Doğa Bilimleri Fakültesi, Kimya Bölümüen_US
dc.description.abstractIn this study, the novel 3-(4-aminopyrimidin-2-ylthio) phthalonitrile (1) as starting material was synthesized and its molecular structure was verified by the experiment of single crystal X-ray diffraction, and it was first brought to the literature. Then, its non-peripherally tetra-substituted phthalocyanines (2,3) and the methylated derivatives (2a,3a) containing cytosine derivative were synthesized herein for the first time. All the compounds used were characterized with various spectroscopic methods such as UV–Vis, FT-IR, 1H NMR, 13C NMR and MALDI-TOF MS by obtaining highly satisfactory results. The acetylcholinesterase inhibitor compounds recorded as important therapeutic drugs for the therapy of Alzheimer's disease. So, these novel phthalocyanines effectively inhibited acetylcholinesterase enzyme, with Ki values in the range of 31.75 ± 5.72 to 107.15 ± 12.67 µM. For this enzyme, IC50 values were obtained in the range of 3.41 ± 0.78 to 10.08 ± 2.65 µM. For ?-glycosidase enzyme, the most effective Ki values of (3) and (3a) were found as 3.41 ± 0.78 and 5.32 ± 1.34 µM, respectively. We used 50 µL substrates for the acetylcholine esterase and ?-glycosidase enzymes and 20 µL enzymes. For AChE, we used distilled water and buffer 800 µL and 100 µL, respectively. Also, we pipetted 500 µL and 300 µL for ?-glycosidase and examined the activities. Indeed, the most potent phthalocyanines against both enzymes were recorded for the purpose to investigate interaction modes of these compounds in the active site of the target enzyme. After treatment of compounds, viability was reduced by approximately 25% in cancer cell lines. The cytotoxicity potential of these phthalocyanines against human breast, colon, and prostate cancers demonstrated that these compounds had normal cytotoxic effects. © 2022 Elsevier B.V.en_US
dc.identifier.citationGünsel, A., Yıldırım, A., Taslimi, P., Erden, Y., Taskin-Tok, T., Pişkin, H., . . . Nilüfer Yarasir, M. (2022). Cytotoxicity effects and biochemical investigation of novel tetrakis-phthalocyanines bearing 2-thiocytosine moieties with molecular docking studies. Inorganic Chemistry Communications, 138 doi:10.1016/j.inoche.2022.109263en_US
dc.identifier.doi10.1016/j.inoche.2022.109263en_US
dc.identifier.issn1387-7003en_US
dc.identifier.scopus2-s2.0-85123778112en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1016/j.inoche.2022.109263
dc.identifier.urihttps://hdl.handle.net/20.500.12713/2463
dc.identifier.volume138en_US
dc.identifier.wosWOS:000788153500004en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.institutionauthorTaslimi, Parham
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofInorganic Chemistry Communicationsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectCrystal Structureen_US
dc.subjectCytotoxicityen_US
dc.subjectEnzyme Inhibitionen_US
dc.subjectMolecular Dockingen_US
dc.subjectPhthalocyanineen_US
dc.subjectSynthesisen_US
dc.titleCytotoxicity effects and biochemical investigation of novel tetrakis-phthalocyanines bearing 2-thiocytosine moieties with molecular docking studiesen_US
dc.typeArticleen_US

Dosyalar

Orijinal paket
Listeleniyor 1 - 1 / 1
Küçük Resim
İsim:
266.pdf
Boyut:
5.9 MB
Biçim:
Adobe Portable Document Format
Açıklama:
Tam Metin / Full Text
İndir
Lisans paketi
Listeleniyor 1 - 1 / 1
Küçük Resim Yok
İsim:
license.txt
Boyut:
1.44 KB
Biçim:
Item-specific license agreed upon to submission
Açıklama:
İndir

Koleksiyon

Scopus İndeksli Yayınlar Koleksiyonu
Kimya Bölümü Makale Koleksiyonu
WoS İndeksli Yayınlar Koleksiyonu