5,7-二氯-8-喹啉醇基-镧系元素的合成、晶体结构、细胞毒性和 DNA 相互作用。
Synthesis, crystal structure, cytotoxicity and DNA interaction of 5,7-dichloro-8-quinolinolato-lanthanides.
机构信息
State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Chemical Engineering of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China.
出版信息
Eur J Med Chem. 2013 Jan;59:194-202. doi: 10.1016/j.ejmech.2012.10.037. Epub 2012 Nov 12.
Four isostructural lanthanide complexes with 5,7-dichloro-8-quinolinoline (H-ClQ): [Sm(ClQ)(3)(H(2)O)(2)]·1.33EtOH·0.33H(2)O (1), [Eu(ClQ)(3)(H(2)O)(2)]·0.5EtOH, (2), [Tb(ClQ)(3)(H(2)O)(2)]·0.5EtOH (3) and [Ho(ClQ)(3)(H(2)O)(2)]·H(2)O (4) were synthesized, in which the lanthanide was coordinated by three ClQ(-) anions and two aqua ligands. The in vitro cytotoxicities of complexes 1-4 against five human tumor cells were evaluated. The IC(50) values of complexes 1-4 against BEL7404, HeLa and A549 were in the range 1.2-6.3, 3.5-6.6 and 10.8-25.2 μM, respectively; except for complex 3 toward BEL7404, they all exhibited enhanced cytotoxicity in comparison to H-ClQ. The binding properties of complexes 1-4 to DNA examined by various methods indicated that complexes 1-4 interacted with DNA more strongly than free quinolinoline, and intercalation was the most probable binding mode for both the complexes and quinolinoline.
四种同构的镧系元素配合物与 5,7-二氯-8-喹啉啉（H-ClQ）：[Sm(ClQ)(3)(H(2)O)(2)]·1.33EtOH·0.33H(2)O（1），[Eu(ClQ)(3)(H(2)O)(2)]·0.5EtOH，（2），[Tb(ClQ)(3)(H(2)O)(2)]·0.5EtOH（3）和[Ho(ClQ)(3)(H(2)O)(2)]·H(2)O（4）被合成，其中镧系元素由三个 ClQ(-)阴离子和两个水配体配位。评估了配合物 1-4 对五种人肿瘤细胞的体外细胞毒性。配合物 1-4 对 BEL7404、HeLa 和 A549 的 IC(50)值分别在 1.2-6.3、3.5-6.6 和 10.8-25.2 μM 的范围内；除了配合物 3 对 BEL7404 之外，与 H-ClQ 相比，它们都表现出增强的细胞毒性。通过各种方法研究了配合物 1-4 与 DNA 的结合特性，表明配合物 1-4 与 DNA 的相互作用比游离喹啉啉更强，并且插入是两种配合物和喹啉啉最可能的结合模式。
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