dc.contributor.author | Kahriman, Nuran | |
dc.contributor.author | Peker, Kıvanç | |
dc.contributor.author | Serdaroğlu, Vildan | |
dc.contributor.author | Aydın, Ali | |
dc.contributor.author | Usta, Asu | |
dc.contributor.author | Fandaklı, Seda | |
dc.contributor.author | Yaylı, Nurettin | |
dc.date.accessioned | 2020-12-19T19:34:34Z | |
dc.date.available | 2020-12-19T19:34:34Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Kahriman, N., Peker, K., Serdaroğlu, V., Aydın, A., Usta, A., Fandaklı, S., & Yaylı, N. (2020). Novel 2-amino-4-aryl-6-pyridopyrimidines and N-alkyl derivatives: Synthesis, characterization and investigation of anticancer, antibacterial activities and DNA/BSA binding affinities. Bioorganic chemistry, 99, 103805. https://doi.org/10.1016/j.bioorg.2020.103805 | en_US |
dc.identifier.issn | 0045-2068 | |
dc.identifier.issn | 1090-2120 | |
dc.identifier.uri | https://doi.org/10.1016/j.bioorg.2020.103805 | |
dc.identifier.uri | https://hdl.handle.net/11436/1124 | |
dc.description | aydin, ali/0000-0002-9550-9111 | en_US |
dc.description | WOS: 000535446600002 | en_US |
dc.description | PubMed: 32272366 | en_US |
dc.description.abstract | A series of new 2-amino-4-aryl-6-pyridopyrimidines, and their N-alkyl bromide derivatives were designed and synthesized by employing methyl substituted azachalcones. These novel compounds were evaluated and compared to the well-known chemotherapeutics in terms of their anti-cancer and anti-microbial functions, and their DNA/protein binding affinities. in order for the cell proliferation, cytotoxicity and microdilution features to be observed, various cancer cell lines (Hep3B, A549, HeLa, C6, HT29, MCF7) were treated with 2-amino-4-aryl-6-pyridopyrimidines (1-9) and their N-alkyl bromide derivatives (2a-c, 3a-c, 5a-c, 6a-c, 8a-c, 9a-c). Studies on the cells revealed that both pyrimidines and their alkyl derivatives (i) have a high anti-proliferative and antimicrobial activities, (ii) cause cell rounding, cytoplasmic blebs, and anomalous globular structure, and (iii) strongly bound to DNA/BSA macromolecules. Especially the length of the alkyl chain of the N-alkyl bromides has an increasing effect on the antiproliferative, antibacterial and cytotoxic functions, also DNA/protein binding affinity. Those results indicate the novel compounds to be promising antiproliferative agents, and their anticancer potential makes them candidates to be used for cancer therapy. | en_US |
dc.description.sponsorship | Karadeniz Technical UniversityKaradeniz Technical University; Scientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [TUBITAK-114R025] | en_US |
dc.description.sponsorship | This study was supported by grants from Karadeniz Technical University and the Scientific and Technological Research Council of Turkey (TUBITAK-114R025). | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Academic Press Inc Elsevier Science | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | 2-Amino-4-aryl-6-pyridopyrimidine | en_US |
dc.subject | N-alkyl bromide | en_US |
dc.subject | Anti-proliferative effect | en_US |
dc.subject | Cytotoxic effect | en_US |
dc.subject | Antibacterial activity | en_US |
dc.subject | DNA/protein binding affinity | en_US |
dc.title | Novel 2-amino-4-aryl-6-pyridopyrimidines and N-alkyl derivatives: Synthesis, characterization and investigation of anticancer, antibacterial activities and DNA/BSA binding affinities | en_US |
dc.type | article | en_US |
dc.contributor.department | RTEÜ, Fen - Edebiyat Fakültesi, Kimya Bölümü | en_US |
dc.contributor.institutionauthor | Usta, Asu | |
dc.identifier.doi | 10.1016/j.bioorg.2020.103805 | |
dc.identifier.volume | 99 | en_US |
dc.relation.journal | Bioorganic Chemistry | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |