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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >DNA targeting half sandwich Ru(ii)-p-cymene-N boolean AND N complexes as cancer cell imaging and terminating agents: influence of regioisomers in cytotoxicity
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DNA targeting half sandwich Ru(ii)-p-cymene-N boolean AND N complexes as cancer cell imaging and terminating agents: influence of regioisomers in cytotoxicity

机译:DNA靶向半三明治Ru(ii)-p-cymenee-n Boolean和n个复合物作为癌细胞成像和终止剂:测定的细胞毒性的影响

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摘要

For diagnosing and annihilating cancer in the human body, herein, we have adopted a one pot convenient synthetic protocol to synthesize a library of half sandwich Ru(ii)-p-cymene-N<^>N complexes under continuous sonication and isolated their regioisomers by preparative thin layer chromatography followed by justification of stability using DFT. The present work has resulted in a library of ruthenium arene complexes and their isolated regioisomers following environmentally benign green processes and their screening of anticancer activity in terms of cytotoxicity and selectivity against cancer cell lines where [(eta(6)-p-cymene)RuCl{2-(5,6-dichloro-1H-benzo[d]imidazole-2-yl)quinolone}] (11j) has been elicited to be significantly more potent as well as selective in Caco-2 and HeLa cell lines than the normal HEK-293 cell line compared to cisplatin and it has even shown marked cytotoxicity against the more aggressive HT-29 colorectal cancer cell line being capable of producing oxidative stress or arresting the cell cycle. Moreover, these types of Ru(ii)-arene complexes exhibited excellent binding efficacy with DNA and the compounds [(eta(6)-p-cymene)RuCl{5-chloro-2-(6-(4-chlorophenyl)pyridin-2-yl)benzo[d]thiazole}]PF6 (8l4), [(eta(6)-p-cymene)Ru-2-(6-(benzofuran-2-yl)pyridin-2-yl)-5-chlorobenzo[d]thiazole (8l9) and [(eta(6)-p-cymene)RuCl{2-(6-nitro-1H-benzo[d]imidazol-2-yl)quinolone}]Cl (11f ') and might be applied for cancer theranostic treatment due to their good fluorescence properties and remarkable potency.
机译:为了诊断和消灭人体内的癌症,本文采用一锅法简便合成方案,在连续超声作用下合成了半三明治Ru(ii)-对-聚伞花序-N<^>N络合物库,并通过制备性薄层色谱分离其区域异构体,然后使用DFT验证稳定性。目前的工作已经形成了一个钌芳烃配合物库及其分离的区域异构体,这些配合物遵循环境友好的绿色工艺,并根据对癌细胞系的细胞毒性和选择性筛选抗癌活性,其中,[(eta(6)-对伞花烯)RuCl{2-(5,6-二氯-1H-苯并[d]咪唑-2-基)喹诺酮](11j)的活性显著更高与顺铂相比,它在Caco-2和HeLa细胞系中比正常的HEK-293细胞系具有更强的选择性,并且对更具攻击性的HT-29结直肠癌细胞系具有显著的细胞毒性,能够产生氧化应激或阻止细胞周期。此外,这些类型的钌(ii)-芳烃络合物与DNA和化合物[(eta(6)-对甲苯)RuCl{5-氯-2-(6-(4-氯苯基)吡啶-2-基)苯并[d]噻唑}]PF6(8l4)表现出优异的结合效率,[(eta(6)-p-异丙基甲苯)Ru-2-(6-(苯并呋喃-2-基)吡啶-2-基)-5-氯苯并[d]噻唑(8l9)和[(eta(6)-p-异丙基甲苯)RuCl{2-(6-硝基-1H-苯并[d]咪唑-2-基)喹诺酮]Cl(11f'),由于其良好的荧光性质和显著的效力,可能被应用于癌症治疗。

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