کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1399854 1501216 2008 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, cytotoxicity and DNA binding levels of tri-functional mononuclear platinum(II) complexes
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis, cytotoxicity and DNA binding levels of tri-functional mononuclear platinum(II) complexes
چکیده انگلیسی

Seven new tri-functional mononuclear platinum(II) complexes (a–g) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV and 1H NMR spectral techniques. The cytotoxicity of these complexes was tested by MTT and SRB assays. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP-MS. The results indicate that the complexes (a–g) have selectivity against tested carcinoma cell lines; they have weaker cytotoxicity against HCT-8 and MCF-7. Complexes a, b, d and g also exert weaker cytotoxicity against BGC-823 and complexes a, b, e and f have better cytotoxicity against EJ, but their cytotoxicity is weaker than that of cisplatin. Complexes c, e and f, confer substantially greater cytotoxicity against HL-60 with an IC50 value of 7.68 ± 0.23, 3.87 ± 0.19 and 2.41 ± 0.18 μM, respectively, moreover, cytotoxicity of complex f is equal to that of cisplatin. Complexes c, e and f cause significant G2/M arrest and a concomitant decrease of cell population in G1 and S phases. The total DNA-platination levels of them are higher than that of cisplatin under the same experimental conditions. It suggests that there is no correlation between total DNA-platination levels in HL-60 cells and cytotoxicity of complexes. When leaving groups are aromatic carboxylates, the complexes have better cytotoxicity, moreover, the substituent in benzene ring also influences cytotoxicity. In addition, when leaving groups are dicarboxylates, dicarboxylates coordinating with platinum through oxygen atoms form different chelate cycle and cycle size also affects their cytotoxicity.

Seven new tri-functional mononuclear platinum(II) complexes (a–g) have been synthesized. The cytotoxicity of the complexes was tested by MTT and SRB assays. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP-MS.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 43, Issue 2, February 2008, Pages 441–447
نویسندگان
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