Richter Stefan, Singh Sushma, Draca Dijana, Kate Anup, Kumbhar Anupa, Kumbhar Avinash S, Maksimovic-Ivanic Danijela, Mijatovic Sanja, Lönnecke Peter, Hey-Hawkins Evamarie
Universität Leipzig, Institut für Anorganische Chemie, Johannisallee 29, 04103 Leipzig, Germany.
Department of Chemistry, Savitribai Phule Pune University, Pune-411007, India.
Dalton Trans. 2016 Aug 16;45(33):13114-25. doi: 10.1039/c6dt01782g.
A series of Ru(II) arene complexes of mono- and bidentate N-donor ligands with carboxyl or ester groups and chlorido ancillary ligands were synthesised and structurally characterised. The complexes have a distorted tetrahedral piano-stool geometry. The binding interaction was studied with calf thymus DNA (CT-DNA) by absorption titration, viscosity measurement, thermal melting, circular dichroism, ethidium bromide displacement assay and DNA cleavage of plasmid DNA (pBR322), investigated by gel electrophoresis. The dichlorido complexes bind covalently to DNA in the dark, similar to cisplatin, while the monochlorido complexes bind covalently on irradiation, similar to cisplatin analogues. The compounds are selectively cytotoxic against several tumour cell lines and show specific nonlinear correlation between dose and activity. This phenomenon is closely related to their potential to act preferentially as inhibitors of cell division.
合成并通过结构表征了一系列含有羧基或酯基的单齿和双齿氮供体配体以及氯辅助配体的钌（II）芳烃配合物。这些配合物具有扭曲的四面体钢琴凳几何结构。通过吸收滴定、粘度测量、热变性、圆二色性、溴化乙锭置换试验研究了与小牛胸腺DNA（CT-DNA）的结合相互作用，并通过凝胶电泳研究了质粒DNA（pBR322）的DNA切割。二氯配合物在黑暗中与DNA共价结合，类似于顺铂，而一氯配合物在光照下共价结合，类似于顺铂类似物。这些化合物对几种肿瘤细胞系具有选择性细胞毒性，并且在剂量和活性之间显示出特定的非线性相关性。这种现象与其优先作为细胞分裂抑制剂的潜力密切相关。
