Lamotrigine derivatives-synthesis, anti-cancer, and anti-MDR-bacterial activities

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dc.authorid0000-0002-1423-0435
dc.contributor.authorKhan, Mahroza Kanwal
dc.contributor.authorSiddiqui, Hina
dc.contributor.authorSharif, Ruby
dc.contributor.authorGüzel, Mustafa
dc.contributor.authorWahab, Atia-tul
dc.contributor.authorYousuf, Sammer
dc.contributor.authorChoudhary, M. Iqbal
dc.date.accessioned2022-06-03T06:23:07Z
dc.date.available2022-06-03T06:23:07Z
dc.date.issued2022
dc.departmentİstanbul Medipol Üniversitesi, Sağlık Bilimleri Enstitüsü, Moleküler Tıp ve Biyoteknoloji Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Rektörlük, Sağlık Bilim ve Teknolojileri Araştırma Enstitüsü
dc.departmentİstanbul Medipol Üniversitesi, Uluslararası Tıp Fakültesi, Dahili Tıp Bilimleri Bölümü, Tıbbi Farmakoloji Ana Bilim Dalı
dc.description.abstractA new series of quaternary ammonium salts 3–21 of lamotrigine (6-(2, 3-dichlorophenyl)-1, 2, 4-triazine-3, 5-diamine) was synthesized via N-alkylation of lamotrigine using different benzyl bromides. The new analogues were characterized by using FT-IR, NMR, and mass spectrometric techniques. Single-crystal X-ray diffraction analysis of compound 10 was also carried out to confirm the position of substitution and salt formation. All the compounds 3-21 were tested for various biological activities, including anti-bacterial, and anti-cancer properties. All compounds, except 20, exhibited a potent growth inhibition of Staphylococcus aureus strains as compared to the ofloxacin, the standard drug. Compounds 4, 7, 10, and 13 showed a significant toxicity towards HeLa cell line (derived from cervical carcinoma), whereas compounds 3, and 5 showed a significant activity towards HeLa, MCF-7 (estrogen and progesterone positive breast cancer cell line), and MDA-MB cell lines (epithelial, human breast cancer cell line), as compared to the standard drug doxorubicin. To the best of our knowledge all analogues of 6-(2, 3-dichlorophenyl)-1, 2, 4-triazine-3, 5-diamine, and their activity against MDR, and anti-cancer is reported here for the first time.
dc.description.sponsorshipSearle Pharmaceuticals Pakistan Ltden_US
dc.identifier.citationKhan, M. K., Siddiqui, H., Sharif, R., Güzel, M., Wahab, A., Yousuf, S. ... Choudhary, M. I. (2022). Lamotrigine derivatives-synthesis, anti-cancer, and anti-MDR-bacterial activities. Journal of Molecular Structure, 1264. https://doi.org/10.1016/j.molstruc.2022.133277
dc.identifier.doi10.1016/j.molstruc.2022.133277
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85130781194
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2022.133277
dc.identifier.urihttps://hdl.handle.net/20.500.12511/9489
dc.identifier.volume1264
dc.identifier.wos000806504900008en_US
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorGüzel, Mustafa
dc.language.isoen
dc.publisherElsevier B.V.
dc.relation.ispartofJournal of Molecular Structureen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectAnti-Bacterial Activity
dc.subjectBreast Cancer
dc.subjectCancer Cell Lines
dc.subjectCytotoxicity
dc.subjectHela
dc.subjectLamotrigine
dc.subjectMCF-7
dc.subjectMDA-MB
dc.subjectQuaternary Ammonium Salts
dc.subjectStaphylococcus Aureus
dc.titleLamotrigine derivatives-synthesis, anti-cancer, and anti-MDR-bacterial activities
dc.typeArticle

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