Academic Journal
Cytotoxicity and DNA binding property of phenanthrene imidazole with polyglycol side chains
| العنوان: | Cytotoxicity and DNA binding property of phenanthrene imidazole with polyglycol side chains |
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| المؤلفون: | Wang, Shuxiang, Li, Hongdong, Chen, Chao, Zhang, Jinchao, Li, Shenghui, Qin, Xinying, Li, Xiaoliu, Wang, Kerang |
| المصدر: | Bioorganic and Medicinal Chemistry Letters |
| بيانات النشر: | Pergamon-Elsevier Ltd |
| المجموعة: | Australian National University: ANU Digital Collections |
| مصطلحات موضوعية: | Keywords: cisplatin, DNA, imidazole derivative, phenanthrene derivative, phenanthrene imidazole derivative, unclassified drug, article, cancer cell culture, drug cytotoxicity, drug DNA binding, drug structure, drug synthesis, reaction analysis, structure analysis, Binding property, Cytotoxicity, Phenanthrene imidazole derivatives, Polyglycol side chain |
| الوصف: | A series of phenanthrene imidazole with polyglycol side chain (2a-2c and 3a-3c) were synthesized and characterized by IR, NMR and MS. The cytotoxicity of 2a-2c and 3a-3c against cancer cell lines (HL-60, BGC-823, Bel-7402 and KB) in vitro were measured using MTT method. The DNA binding properties of 3a-3c were investigated by UV, fluorescence, CD spectroscopies and thermal denaturation. The results indicate that 2a exhibits higher cytotoxicity than cisplatin against BGC-823 and Bel-7402 cell lines, 3b and 3c exhibit higher cytotoxicity than 2b and 2c against BGC-823, Bel-7402 and KB cell lines. The cytotoxic effect of 2a-2c decrease with the increase of side chains length, the cytotoxic effect of 3a-3c increased with the increasing length of side chains against BGC-823, Bel-7402 and KB cell lines. Compounds 3a-3c intercalated DNA with a vertical orientation in the intercalation pocket. The binding constants of 3a-3c with Ct-DNA are 1.68 × 106, 1.51 × 106 and 0.709 × 106 M-1, respectively. The binding affinity of 3a-3c with Ct-DNA trended to decrease with the increasing length of polyglycol side chains. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | unknown |
| تدمد: | 0960-894X |
| Relation: | http://hdl.handle.net/1885/78281; https://openresearch-repository.anu.edu.au/bitstream/1885/78281/5/f5625xPUB69502012.pdf.jpg; https://openresearch-repository.anu.edu.au/bitstream/1885/78281/7/01_Wang_Cytotoxicity_and_DNA_binding_2012.pdf.jpg |
| DOI: | 10.1016/j.bmcl.2012.08.079 |
| الاتاحة: | http://hdl.handle.net/1885/78281 https://doi.org/10.1016/j.bmcl.2012.08.079 https://openresearch-repository.anu.edu.au/bitstream/1885/78281/5/f5625xPUB69502012.pdf.jpg https://openresearch-repository.anu.edu.au/bitstream/1885/78281/7/01_Wang_Cytotoxicity_and_DNA_binding_2012.pdf.jpg |
| رقم الانضمام: | edsbas.848B26B4 |
| قاعدة البيانات: | BASE |
| تدمد: | 0960894X |
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| DOI: | 10.1016/j.bmcl.2012.08.079 |