dc.contributor.author | Khan, Mahroza Kanwal | |
dc.contributor.author | Siddiqui, Hina | |
dc.contributor.author | Sharif, Ruby | |
dc.contributor.author | Güzel, Mustafa | |
dc.contributor.author | Wahab, Atia-tul | |
dc.contributor.author | Yousuf, Sammer | |
dc.contributor.author | Choudhary, M. Iqbal | |
dc.date.accessioned | 2022-06-03T06:23:07Z | |
dc.date.available | 2022-06-03T06:23:07Z | |
dc.date.issued | 2022 | en_US |
dc.identifier.citation | Khan, 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 | en_US |
dc.identifier.issn | 0022-2860 | |
dc.identifier.issn | 1872-8014 | |
dc.identifier.uri | https://doi.org/10.1016/j.molstruc.2022.133277 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12511/9489 | |
dc.description.abstract | A 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. | en_US |
dc.description.sponsorship | Searle Pharmaceuticals Pakistan Ltd | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Elsevier B.V. | en_US |
dc.rights | info:eu-repo/semantics/embargoedAccess | en_US |
dc.subject | Anti-Bacterial Activity | en_US |
dc.subject | Breast Cancer | en_US |
dc.subject | Cancer Cell Lines | en_US |
dc.subject | Cytotoxicity | en_US |
dc.subject | Hela | en_US |
dc.subject | Lamotrigine | en_US |
dc.subject | MCF-7 | en_US |
dc.subject | MDA-MB | en_US |
dc.subject | Quaternary Ammonium Salts | en_US |
dc.subject | Staphylococcus Aureus | en_US |
dc.title | Lamotrigine derivatives-synthesis, anti-cancer, and anti-MDR-bacterial activities | en_US |
dc.type | article | en_US |
dc.relation.ispartof | Journal of Molecular Structure | en_US |
dc.department | İstanbul Medipol Üniversitesi, Sağlık Bilimleri Enstitüsü, Moleküler Tıp ve Biyoteknoloji Ana Bilim Dalı | en_US |
dc.department | İstanbul Medipol Üniversitesi, Rektörlük, Sağlık Bilim ve Teknolojileri Araştırma Enstitüsü | en_US |
dc.department | İstanbul Medipol Üniversitesi, Uluslararası Tıp Fakültesi, Dahili Tıp Bilimleri Bölümü, Tıbbi Farmakoloji Ana Bilim Dalı | en_US |
dc.authorid | 0000-0002-1423-0435 | en_US |
dc.identifier.volume | 1264 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.identifier.doi | 10.1016/j.molstruc.2022.133277 | en_US |
dc.institutionauthor | Güzel, Mustafa | |
dc.identifier.wosquality | Q3 | en_US |
dc.identifier.wos | 000806504900008 | en_US |
dc.identifier.scopus | 2-s2.0-85130781194 | en_US |
dc.identifier.scopusquality | Q2 | en_US |