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DNA Interactions and Antiproliferative Activity Studies of Octahedral Nickel Complexes of Two Extended Phenanthrolines
ChemistrySelect ( IF 1.9 ) Pub Date : 2021-09-09 , DOI: 10.1002/slct.202102376 Burak Coban 1 , Engin Saka 1 , Ufuk Yıldız 1 , Senem Akkoç 2
ChemistrySelect ( IF 1.9 ) Pub Date : 2021-09-09 , DOI: 10.1002/slct.202102376 Burak Coban 1 , Engin Saka 1 , Ufuk Yıldız 1 , Senem Akkoç 2
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Two new imidazophenanthroline derivatives, namely 2-(4-bromo-(2,1,3)-benzothiadiazol-7-yl)-1H-imidazo[4,5-f][1,10]phenanthroline (btdip), 2-(dibenzofuran-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline (dbfip) and their octahedral nickel complexes [Ni(phen)2(btdip)]2+ (1) and [Ni(phen)2(dbfip)]2+ (2) have been synthesized and characterized by CHN analysis, ESI-MS, NMR and UV-vis spectra. Their DNA binding abilities were spectrophotometrically, hydrodynamically and electrophoretically studied and found that while btdip binds DNA externally, dbfip binds in the grooves and both of their nickel complexes also bind DNA through grooves giving severe DNA damage in the presence of peroxide. The compounds were screened against four different human cancer cell lines using MTT assay method. The results obtained showed that both ligands are active against DLD-1, and further dbfip is found to be more active than positive control drugs against DLD-1 and HepG2 cell lines. The complex 2 has more antiproliferative effect than 1 against MCF-7 and HepG2 cells. On the other hand, complex 2 was found to have more toxic effect on HepG2 cells than the standard drugs cisplatin and ploxal-S.
中文翻译：
两种扩展菲咯啉八面体镍配合物的 DNA 相互作用和抗增殖活性研究
两种新的咪唑并菲咯啉衍生物，即 2-(4-bromo-(2,1,3)-benzothiadiazol-7-yl)-1 H - imidazo [4,5- f ][1,10]phenanthroline ( btdip ), 2 -(dibenzofuran-3-yl)-1 H -imidazo [4,5- f ][1,10] 菲咯啉 ( dbfip ) 及其八面体镍配合物 [Ni(phen) 2 (btdip)] 2+ ( 1 ) 和[Ni(phen) 2 (dbfip)] 2+ ( 2 ) 已合成并通过 CHN 分析、ESI-MS、NMR 和 UV-vis 光谱表征。通过分光光度法、流体动力学和电泳法研究了它们的 DNA 结合能力，发现btdip在外部结合 DNA，dbfip在凹槽中结合，它们的两种镍复合物也通过凹槽结合 DNA，在过氧化物存在的情况下造成严重的 DNA 损伤。使用 MTT 分析方法针对四种不同的人类癌细胞系筛选化合物。获得的结果表明，这两种配体都对 DLD-1 具有活性，并且进一步发现dbfip比阳性对照药物对 DLD-1 和 HepG2 细胞系的活性更高。复合物2对 MCF-7 和 HepG2 细胞的抗增殖作用比复合物1 强。另一方面，发现复合物2对 HepG2 细胞的毒性作用比标准药物顺铂和 ploxal-S 更强。
更新日期：2021-09-10
中文翻译：
两种扩展菲咯啉八面体镍配合物的 DNA 相互作用和抗增殖活性研究
两种新的咪唑并菲咯啉衍生物，即 2-(4-bromo-(2,1,3)-benzothiadiazol-7-yl)-1 H - imidazo [4,5- f ][1,10]phenanthroline ( btdip ), 2 -(dibenzofuran-3-yl)-1 H -imidazo [4,5- f ][1,10] 菲咯啉 ( dbfip ) 及其八面体镍配合物 [Ni(phen) 2 (btdip)] 2+ ( 1 ) 和[Ni(phen) 2 (dbfip)] 2+ ( 2 ) 已合成并通过 CHN 分析、ESI-MS、NMR 和 UV-vis 光谱表征。通过分光光度法、流体动力学和电泳法研究了它们的 DNA 结合能力，发现btdip在外部结合 DNA，dbfip在凹槽中结合，它们的两种镍复合物也通过凹槽结合 DNA，在过氧化物存在的情况下造成严重的 DNA 损伤。使用 MTT 分析方法针对四种不同的人类癌细胞系筛选化合物。获得的结果表明，这两种配体都对 DLD-1 具有活性，并且进一步发现dbfip比阳性对照药物对 DLD-1 和 HepG2 细胞系的活性更高。复合物2对 MCF-7 和 HepG2 细胞的抗增殖作用比复合物1 强。另一方面，发现复合物2对 HepG2 细胞的毒性作用比标准药物顺铂和 ploxal-S 更强。
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